If not otherwise indicated, cells were pretreated with I-BET151, iBET-BD1, iBET-BD2 or vehicle (DMSO) for 48 hours, irradiated with 0 or 6 Gy, and incubated for additional time intervals with concurrent drug. CAS Number: 2451862-42-1. Its mechanism of action is not fully understood. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 Hydrochloride. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. amni) under a material transfer agreement with GSK. BET BD1 related products. Email. , 2013). Available to order from Sigma-Aldrich. 6147. GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. 22 Early preclinical results demonstrate different phenotypic responses from domain-selective BET inhibitors and reduced toxicity when using pan-BET BD2 selective inhibitors. 1 μg/mL, which we determined was the equivalent of 1000 units/mL (U/mL) via in-house. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. - Mechanism of Action & Protocol. 1B, fig. CTB ( Cholera Toxin B subunit ) Catalog No. ABBV-744 is highly selective for BD2 of BRD2, BRD3 and BRD4, 64 exhibiting several hundred-fold higher affinity for the BD2 over BD1. Chemical Structure GSK778. GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. Available to order from Sigma-Aldrich. Email. All Photos (1) Documents. ZA EN. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). All products from TargetMol are for Research Use Only. Fax: +1 510. Email. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains outside of. Download scientific diagram | Correlations of protein vibrational entropy between standard NMA and scaled coarsegrained NMAs: a) sBNM, b) sGNM, and c) sANM. COO/ COA. 5), is a highly selective BD1 inhibitor (BRD4(1), IC 50 = 41 nM) with a 143-fold selectivity over BD2. ChemicalBook あなたのためにGSK778(2451862-42-1)の化学的性質を提供して、融点、価格、蒸気圧、沸点、毒性、比重、沸点、密度、分子式、分子量、物理的な性質、毒性 税関のコードなどの情報、同時にあなたは更にGSK778(2451862-42-1)の製品の全世界の供給商にブラウズすることができて、生産企業と生産. GD EN. 10 µM; GSK791. All Photos (1) Documents. Recombinant IL-1β (Peprotech, Cranbury, NJ) was reconstituted RPMI at 0. WGK. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046 affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 . To date, 61 bromodomains have been identified in 46 diverse proteins in human cells (Filippakopoulos et al. Copy Link. Applications Products Services Documents Support. All. SML3234. Drug Formulation: This drug may be formulated in DMSO. ≥98% (HPLC)Shop Medchemexpress LLC HY-136570 5mg , GSK778 CAS:2451862-42-1 Purity:>98% at Fishersci. 5. 26 (n= 10); 40-fold. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models[1]. GSK778 Hydrochloride. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. All Photos (1) Documents. , 2021). Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET‐BD1 (GSK778) and iBET‐BD2 (GSK046)). WGK. 0. WGK 3. Selectivity profile of I-BET151, iBET-BD1 (GSK778) and iBET-BD2 (GSK046). SML3234. Email. SML3234. 2451862-42-1: Formula: C 30 H 33 N 5 O 3: Formula Wt. Código de clase de almacenamiento. Available to order from Sigma-Aldrich. Available to order from Sigma-Aldrich. WGK 3. SERP Rating Probe GSK778 is in the process of SERP review. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. GSK778 Hydrochloride. Meanwhile, GSK778 has IC 50 s of 75 nM. Email. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046 affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 . Here, we report two unexpected findings: (1) SynGRs bearing pan-BET or BD2-selective ligands license transcription at the FXN locus, whereas those bearing BD1-selective ligands do not, and (2) rather than being neutral or inhibitory, an untethered BD1-selective ligand (GSK778) substantively enhances the activity of all active SynGRs. 7 B) indicated that GSK778 maintains all of the critical interactions of I-BET151 with BRD4-BD1, including the hydrogen bonding interaction of the 3,5-dimethylisoxazole moiety with the conserved Asn140, the hydrophobic interaction of the aryl ring of the α-methylbenzyl group with the. GSK778 Hydrochloride. GB EN. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 9 BRD: BAZ2A/2B: BAZ2-ICR. CAS Number: 2451862-42-1. On the basis of sequence homology, BCPs are classified into eight different subgroups (families). GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 5 (LPS-PBMC assay) ≤ 10 µM. Available to order from Sigma-Aldrich. 33DFTG (TD139) $21. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Applications Products Services Documents Support. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Buy Epigenetic Reader Domain inhibitor GSK778 (iBET-BD1) from. Buy Epigenetic Reader Domain inhibitor GSK778 (iBET-BD1) from AbMole BioScience. 6SWN, 6SWO, 6SWP, 6SWQ. Structural Genomics Consortium MaRS Centre, South Tower 101 College St. Phylogenetic tree of the human bromodomain-containing protein subgroups. All Photos (1) Documents. Email. Primary Citation of Related Structures: 6SWN, 6SWO, 6SWP, 6SWQ. Many reports have shown that pan BETis, such as JQ1 and iBET762, exhibited no selectivity between BD1 and BD2, but BD1-selective (GSK778) or BD2-selective (GSK046 and ABBV-744) BETis showed. GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). GSK778 Hydrochloride. toronto@thesgc. GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1 with IC50 of 75 nM (BRD2-BD1), 41 nM (BRD3-BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1),. PL EN. I-BET151, GSK778, GSK046 and GSK620 are available from R. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. SML3234. All Photos (1) Documents. Catalog Number: AA01KEG7. nM, SPR BRD4 (BD1): pKd= 8. GSK778 (iBET-BD1) potently inhibits numerous cancer cells. Email. 65 ABBV-744 shows potent anti-proliferative effects against. Another report showed that BD2-selective BET family inhibitors exhibited good efficacies in treating prostate cancer 22. 13 Similar interactions were found by our recently reported triazole-based inhibitors, including DW34, which exhibit pan-D1 selectivity, with. 9. COO/ COA. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Before sharing sensitive information, make sure you’re on a federal government site. All Photos (1) Documents. from publication: Fast and Accurate. SGC Toronto. 5 mg/dL, except in individuals with Gilbert's syndrome. ([email protected]) and I. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. Available to order from Sigma-Aldrich. GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1). SML3234. 14 GSK778, another pan-D1-selective inhibitor (Figure 1A), was recently reported. Available to order from Sigma-Aldrich. GSK778 phenocopies the. 11 - Combustible Solids. COO/ COA. • (+)-JQ1 has 45–50 times more binding capabilities to BD1 compared with BD2 (Chen et al. 77 The basic structure of BET proteins is comprised of. Shelf Life: >2 years if stored properly. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Email. PubMed Abstract: The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins enable chromatin binding to facilitate transcription. All Photos (1) Documents. BRD3 (BD1) pIC. Safety Information. All Photos (1) SML3234. Safety Information. GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis . Serum alanine aminotransferase (ALT)/aspartate aminotransferase (AST) < 2. Available to order from Sigma-Aldrich. Available to order from Sigma-Aldrich. Copy Link. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Resolution:Description GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 Hydrochloride. Available to order from Sigma-Aldrich. The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. SML3234. SML3234. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. Despite their profound preclinical efficacy, the clinical utility of pan-inhibitors is limited due to observed cytotoxicicities. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. Copy Link. While GSK789 was less selective (TAF1-BD2 K d = 50 nM and TAF1L-BD2 K d = 398 nM), it. , 2016). SML3234. COO/ COA. iBET-BD1 phenocopies the effects of pan-BET inhibitors in cancer models, whereas iBET-BD2 is predominantly effective in. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. Miransertib is an Orally Active Akt Inhibitor for Cancer and Infection Research. All Photos (1) Documents. SML3234. Copy Link. 5 (LPS-PBMC assay) ≤ 10 µM. This approachGSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. ≥98% (HPLC)Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. For research use only. All Photos (1) Documents. GSK778. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Well-characterized small molecules are essential tools for studying the biology and therapeutic relevance of a target protein. Available to order from Sigma-Aldrich. Your information is safe with us. The subsequent development and application of GSK778 (BD1 selective) and GSK046 (BD2 selective) revealed that inhibition of BD2 was ineffective in displacing BET proteins from chromatin. Herein,. Meanwhile, GSK778 has IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. P (moc. +86-21-51987688Crystal structure of GSK778 complexed with BRD4-BD1 (Fig. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778에 대한 모든 정보는 Chemicalbook 에서 조회 할 수 있습니다. Find (s)-1-phenylethyl (r)-acetoxyphenylacetate and related products for scientific research at MilliporeSigmaGSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. $21. COO/ COA. : 2451862-42-1. *. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. (D) Venn diagram showing the overlap between top DCP hits in tumor organoids (ERKi) and normal organoids (BAY-293, BI99179, GSK778, GSK789). Email. Email. All Photos (1) Documents. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1]. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. However, recent reports of potent and selective pan-BET BD1 and pan-BET BD2 inhibitors have been reported including ABBV-744, 21 GSK778, and GSK046. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Figure 4. Applications Products Services Documents Support. GSK778 Hydrochloride. GSK778 Hydrochloride. GSK778 Hydrochloride. Applications Products Services Documents Support. (B). ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. 11 - Combustible Solids. SML3234. WGK 3. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. Immunoblots. Apart from BRDs, YEATS family members have been. In recent years, members of the bromodomain and. Email. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046, affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 [28]. thesgc. iBET-BD1 showed a selectivity of ≥130-fold for BRD4 BD1, and iBET-BD2. GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). 5% gels (100 V, 90 min) and transferred to nitrocellulose membranes (90 V, 90 min). GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and. Given the high sequence similarity amongst BET bromodomains, small molecule inhibitors for a single BET bromodomain are lacking; however, potent pan-D2 inhibitors (e. Email. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. S1F, and table S1). R (moc. GSK778 Hydrochloride. nM, SPR BRD4 (BD1): pKd= 8. 61 bulk manufacturing, sourcing and procurement. 1B, fig. Safety Information. The oldest compound, RVX-208 based on a quinazolinone chemical core, exhibited a selectivity of 20-fold with K D values of 4100 nMComprar GSK778 hydrochloride na CymitQuimica a partir de 187,0 €I-BET151 (GSK1210151A), iBET-BD1 (GSK778) and iBET-BD2 (GSK046) were provided by GlaxoSmithKline plc (GSK, London, UK). , 2020). Domain-Selective Targeting (BD1 or BD2 Targeting) The BET protein family of BCPs comprise the ubiquitously expressed BRD2, BRD3, and BRD4 and the testis-restricted BRDT, all of which harbor two highly conserved tandem bromodomains, BD1 and BD2, allowing them to. Developing BDII selective compounds was far more challenging, and only a handful of BDII selective inhibitors have been developed to date (Figure 1). Figure 4. The bromodomain (BD) is a ~110 amino acid motif that binds to acetyl-lysine modifications on histone and non-histone proteins (Dhalluin et al. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50 s of 75 nM ( BRD2 BD1 ), 41 nM ( BRD3 BD1 ), 41 nM ( BRD4 BD1 ), and 143 nM ( BRDT BD1 ), respectively. This approach Product Description. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. comThe calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. 1 ± 0. COO/ COA. LT EN. Available to order from Sigma-Aldrich. GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. gov means it’s official. Applications Products Services Documents Support. Obviously, GSK778 reduces the clonogenic capacity of primary human AML cells. Louis Gilman November 13, 2023. GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. WGK 3. 3; Cell. The two tandem bromodomains of the BET. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET-BD1 [GSK778] and iBET-BD2 [GSK046]). GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. . Email. First of all, GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. SML3234. E-newsletter Get updates ,discounts and special offers. 1B, fig. First of all,. Email. GSK778 (iBET-BD1) [GSK reference 1, 5] is an analogue of I-BET151 [68] with good potency against BET BD1s (IC 50 s ≈ 40–75 nM) and similar selectivity to LT052 between the BDs of BRD4 (110-fold -to 140-fold depending on assay format), but this selectivity is slightly lower for BRD2 and BRD3 (30–65-fold). COO/ COA. GSK778 phenocopies the. Available to order from Sigma-Aldrich. 2h 41m. 00. SML3234. Visit ChemicalBook To find more GSK484(1652591-81-5) information like chemical properties,Structure,melting point,boiling point,density,molecular formula,molecular weight, physical properties,toxicity information,customs codes. Get latest info on GSK778, suppliers, manufacturers, wholesalers, traders with GSK778 prices for buying. ksg@ajoir. Applications Products Services Documents Support. BET proteins are linked to cancer progression due to their. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. MCP-1 in LPS-stimulated PBMCs: 1000 <1: 32193360. 1B, fig. GSK778 also displayed strong anti-cancer effects in vivo, prolonging the survival of mice carrying an aggressive form of AML at only 15 mg/kg. COO/ COA. Copy Link. Copy Link. 00. Drug Formulation: This drug may be formulated in DMSO. ≥98% (HPLC) All Photos (1)GSK778 (iBET-BD1) هو مثبط قوي وانتقائي BD1 bromodomain لبروتينات BET ، مع IC50s 75 نانومتر (BRD2 BD1) ، 41 نانومتر (BRD3 BD1) ، 41 نانومتر (BRD4 BD1) ، و 143 نانومتر (BRDT BD1) ، على التوالى. e. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. PK EN. Applications Products Services Documents Support. WGK 3. Please continue to check back for new reviews and commentary. (E) Ratio of cell viability in the tumor vs normal is represented in the heat map, where the blue color indicates strong effects in tumor organoids and orange shows pronounced effects in. Copy Link. GSK778 also displayed strong anti-cancer effects in vivo, prolonging the survival of mice carrying an aggressive form of AML at only 15 mg/kg. R. ID EN. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. All Photos (1) Documents. GSK778 phenotyping the role of pan-BET inhibitors in cancer models. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET-BD1 [GSK778] and iBET-BD2 [GSK046]). Open in a separate window. Products are for research use only. GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. Biological Activity：GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. S1F, and table S1). The oldest copound, RVX-208 based on a quinazolinone chemical core, exhibited a selectivity of 20-fold with K D values of 4100 nM andGSK778 (iBET-BD1) BD1 of BET proteins: IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively: Cancer model (mouse) GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. BROMODOMAIN AND EXTRA‐TERMINAL (BET) PROTEINS. The. BD1 selective inhibitors, such as GSK778, MS-436, Olinone, and BI-2536, as well as the BD2 selective inhibitors RVX-208, RVX-297, GSK046, and ABBV-744 have been produced. Products are for research use only. Chemical Structure. Available to order from Sigma-Aldrich. iBET-BD1 dihydrochloride . Copy Link. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 : Catalog Number: M10828: CAS Number: 2451862-42-1: 1. MS EN. 11 - Combustible Solids. R3653. For example, whereas a BD1-selective inhibitor (GSK778) showed similar phenocopies of pan BETis in cancers, a BD2-selective inhibitor (GSK046) showed better effectiveness in inflammatory and autoimmune diseases 2. Catalog Number: AA01KEG7. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Particularly, GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells. Your information is safe with us. (a) Phylogenetic tree of bromodomains, with available chemical probes noted; the BET subfamily and the divergence of its first and second bromodomains, BD1 and BD2, are highlighted (adapted from chromohub. GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. SML3234. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. Forodesine hydrochloride ≥98% (HPLC); Synonyms: 7-[(2S,3S,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one, hydrochloride salt,BCX-1777 HCl,ImmH HCl,Immucillin-H HCl; find Sigma-Aldrich-SML3378 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma. amni) under a material transfer agreement with GSK. PM EN. GSK778. Glatiramer acetate is a mixture of synthetic peptides randomly composed of glutamic acid, lysine, alanine, and tyrosine. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT.