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| Product | Description | |
|---|---|---|
| BET bromodomain inhibitor | A BET bromodomain inhibitor that can be used for the treatment of hematologic malignancies. It binds BET proteins to suppress the interaction between these proteins, propeins and acetylated chromatin, as well as transcription factors. The BET bromodomain inhibitor modulates the expression of oncogenes. Uses: The treatment of hematologic malignancies. Synonyms: MDK3597; MDK-3597; MDK 3597; BET bromodomain inhibitor. 2-[8-Chloro-6-(4-chloro-phenyl)-1-methyl-4H-3-oxa-2,5-diaza-benzo[e]azulen-4-yl]-acetamide. Grades: ≥98%. CAS No. 1505453-59-7. Molecular formula: C20H15Cl2N3O2. Mole weight: 400.259. |  |
| BET bromodomain inhibitor | BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11. Uses: Scientific research. Group: Signaling pathways. CAS No. 1505453-59-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-103036. |  |
| BET bromodomain inhibitor 3 | BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with K i value of > 40 μM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 854137-39-6. Pack Sizes: 10 mg. Product ID: HY-153593. | |
| BET bromodomain inhibitor 4 | BET bromodomain inhibitor 4 (example 7) is an inhibitor of the BET bromodomain domain [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2407658-41-5. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-157393. | |
| 3-Bromo-5-hydroxybenzyl Alcohol | 3-Bromo-5-hydroxybenzyl Alcohol is an intermediate used to prepare (isoxazolylphenyl) arylmethanols as inhibitors of the BET bromodomain family member BRD4(1) for potential use as antitumor agents. Group: Biochemicals. Grades: Highly Purified. CAS No. 1020336-51-9. Pack Sizes: 500mg, 1g. Molecular Formula: C7H7BrO2, Molecular Weight: 203.03. US Biological Life Sciences. |  Worldwide |
| ABBV-744 | ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers. Synonyms: N-ethyl-4-(2-(4-fluoro-2,6-dimethylphenoxy)-5-(2-hydroxypropan-2-yl)phenyl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide. Grades: ≥98%. CAS No. 2138861-99-9. Molecular formula: C28H30FN3O4. Mole weight: 491.55. | |
| Apabetalone | Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC 50 s are 87 μM and 0.51 μM for BD1 and BD2 , respectively [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: RVX-208; RVX000222. CAS No. 1044870-39-4. Pack Sizes: 10 mM * 1 mL; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-16652. | |
| AT 1 | AT 1 is a highly selective BRD4 protein degrader composed of a BET bromodomain inhibitor (+)-JQ1 conjugated to a von Hippel-Lindau (VHL) ligand. Synonyms: BRD4 degrader AT1; (2S,4R)-1-((R)-2-acetamido-3-((6-(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)hexyl)thio)-3-methylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide. Grades: ≥98%. CAS No. 2098836-45-2. Molecular formula: C48H58ClN9O5S3. Mole weight: 972.68. | |
| AZD5153 | AZD5153 (Compound 13) is a trivalent triazolpyrazine bromide domain (BRD), bromodomain and extraterminal (BET) inhibitor. AZD5153 has down-regulated c-Myc gene and tumor growth inhibition activity. AZD5153 can be used in the study of BET small molecule inhibitors [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1869912-39-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg. Product ID: HY-100653. | |
| AZD 5153 | AZD5153 is a potent, selective, and orally available inhibitor of the bromodomain and extraterminal (BET) Inhibitor. It can simultaneously bind two bromodomains in BRD4 with the IC50 value of 5 nM, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma. AZD5153 also shows enhanced potency as a result of bivalent binding and a clear correlation between BRD4 activity and cellular potency. Synonyms: (3R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidinyl]phenoxy]ethyl]-1,3-dimethyl-2-piperazinone; (3R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-1,3-dimethylpiperazin-2-one. Grades: ≥ 95 %. CAS No. 1869912-39-9. Molecular formula: C25H33N7O3. Mole weight: 479.57. | |
| AZD5153 6-Hydroxy-2-naphthoic acid | AZD5153 6-Hydroxy-2-naphthoic acid, a 6-hydroxy-2-naphthoic acid salt of AZD-5153, is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor possessing a bivalent binding mode (pKi = 8.3 for BRD4). Synonyms: AZD5153 6-Hydroxy-2-naphthoic acid; AZD 5153 6-Hydroxy-2-naphthoic acid; AZD-5153 6-Hydroxy-2-naphthoic acid; 6-hydroxynaphthalene-2-carboxylic acid;4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-1,3-dimethylpiperazin-2-one. CAS No. 1869912-40-2. Molecular formula: C36H41N7O6. Mole weight: 667.75. | |
| AZD5153 6-Hydroxy-2-naphthoic acid | AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC 50 of 1.7 nM. Uses: Scientific research. Group: Signaling pathways. CAS No. 1869912-40-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-100653A. | |
| BET-IN-1 | BET-IN-1, an oxazole derivative, can be used as a bromodomain inhibitor. Synonyms: 4-[8-methoxy-1-[(2R)-1-methoxypropan-2-yl]-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazoleBET-IN-1; BET IN 1SCHEMBL14698278CS-5464; HY-19760; CS 5464; HY 19760; CS5464; HY19760. CAS No. 1422554-34-4. Molecular formula: C25H30N4O4. Mole weight: 450.53. | |
| BI-9564 | BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 ?M and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 ?M for BET family[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1883429-22-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-100352. | |
| BMS-986158 | BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins with potential antineoplastic activity. Synonyms: 2-[3-(3,5-dimethyltriazol-4-yl)-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol; BMS-986158; BMS 986158; BMS986158. CAS No. 1800340-40-2. Molecular formula: C30H33N5O2. Mole weight: 495.62. | |
| CF53 | CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K i of <1 nM, K d of 2.2 nM and an IC 50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1808160-52-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-112610. | |
| CPI203 | CPI203, also known as TEN010, JQ-2; RO6870810 and RG6146, is a potent and orally active BET bromodomain inhibitor. CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. CPI203 ownregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. CPI203 arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). Uses: Designed for use in research and industrial production. Additional or Alternative Names: CPI203; CPI-203; CPI 203; TEN010; TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RG 6146; RG-6146; RO6870810; RO-6870810; RO 6870810. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1446144-04-2. Molecular formula: C19H18ClN5OS. Mole weight: 399.9. Purity: >98%. IUPACName: (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide. Canonical SMILES: O=C(N)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1. Product ID: ACM1446144042. Alfa Chemistry ISO 9001:2015 Certified. |  |
| CPI-203 | CPI-203 is a BET bromodomain inhibitor. It inhibits BRD4 in vitro and in cells, and causes G1 cell cycle arrest. It also arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). Synonyms: CPI203; CPI-203; CPI 203; TEN010; TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RG 6146; RG-6146; RO6870810; RO-6870810; RO 6870810. (6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide. Grades: >98%. CAS No. 1446144-04-2. Molecular formula: C19H18ClN5OS. Mole weight: 399.90. | |
| CPI-203 | CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 ?-screen assay). Uses: Scientific research. Group: Signaling pathways. CAS No. 1446144-04-2. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-15846. | |
| CPI-637 | CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively. CPI-637 displayed a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50=11.0 ± 0.6 μM). Synonyms: CPI-637; CPI 637; CPI637. (4R)-4-methyl-6-[1-methyl-3-(1-methylpyrazol-4-yl)indazol-5-yl]-1,3,4,5-tetrahydro-1,5-benzodiazepin-2-one; CPI-637; SCHEMBL17673230. Grades: >98%. CAS No. 1884712-47-3. Molecular formula: C22H22N6O. Mole weight: 386.459. | |
| GSK046 | GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity[1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: iBET-BD2. CAS No. 2474876-09-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136571. | |
| GSK525762 | GSK525762A, also known as I-BET-762 and GSK525762, is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity. Upon administration, the BET inhibitor GSK525762 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, BET proteins, comprising of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth. Synonyms: GSK525762; GSK525762; GSK525762; GSK525762A; GSK-525762A; GSK 525762A; I-BET-762; I-BET762; I-BET 762; molibresib. CAS No. 1260907-17-2. Molecular formula: C22H22ClN5O2. Mole weight: 423.9. | |
| GSK 525768A | GSK 525768A is a enantiomer analogue of GSK 525762A which is a BET family inhibitor aiming at the bromodomain and has potential effect against cancers and sorts of other diseases related to BET bromodomains. Uses: Gsk 525768a is a enantiomer analogue of gsk 525762a which is a bet family inhibitor aiming at the bromodomain and has potential effect against cancers and sorts of other diseases related to bet bromodomains. Synonyms: GSK 525768A; GSK525768A; GSK-525762A; CHEMBL2153435; SCHEMBL12966358; DTXSID50680634. Grades: 98%. CAS No. 1260530-25-3. Molecular formula: C22H22ClN5O2. Mole weight: 423.90. | |
| GSK5959 | GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 value of 80 nM. It exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. It is used at 10 μM final concentration in various in vitro assays. It disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3 in vitro. Uses: Gsk-5959 disrupts chromatin binding of brpf1 in a cellular assay. Synonyms: N-(1,3-dimethyl-2-oxo-6-piperidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide;GSK-5959; GSK 5959; GSK5959. Grades: >98%. CAS No. 901245-65-6. Molecular formula: C22H26N4O3. Mole weight: 394.47. | |
| GSK620 | GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2088410-46-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-137892. | |
| GSK778 | 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 phenocopies the effects of pan-BET inhibitors in cancer models[1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: iBET-BD1. CAS No. 2451862-42-1. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136570. | |
| GW841819X | GW841819X, a benzodiazepin derivative, has been found to be a BET bromodomains inhibitor that could be probably significant in the study of myeloma and leukemia at some extent. Synonyms: KB-75882; KB 75882; KB75882; benzyl (1-methyl-6-phenyl-4hbenzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)carbamate. Grades: 98%. CAS No. 146135-18-4. Molecular formula: C25H21N5O2. Mole weight: 423.48. | |
| I-BET151 | I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4 , BRD2 , and BRD3 with pIC 50 of 6.1, 6.3, and 6.6, respectively [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: GSK1210151A. CAS No. 1300031-49-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13235. | |
| I-BET151 | I-BET151 is a BET bromodomain inhibitor, which blocks recruitment of BET to chromatin. It was shown to induce early cell cycle arrest and apoptosis in human and mouse MLL-fusion leukemia cell lines. Synonyms: GSK1210151A; 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one. Grades: >98%. CAS No. 1300031-49-5. Molecular formula: C23H21N5O3. Mole weight: 415.453. | |
| I-BET 151 dihydrochloride | The hydrochloride salt form of I-BET 151, which has been found to be a BET bromodomain inhibitor and exhibit activities against human and murine MLL-fusion leukaemic cell lines. Synonyms: I-BET 151 dihydrochloride; I BET 151 dihydrochloride; IBET 151 dihydrochloride; IBET151 dihydrochloride; 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydroxy-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1883545-47-8. Molecular formula: C23H21N5O3.2HCl. Mole weight: 488.37. | |
| INCB054329 | INCB054329 is a novel bromodomain and extraterminal domain (BET) inhibitor. It induces vulnerabilities in myeloma cells by inhibition of BET protein. Uses: Antineoplastic agents. Synonyms: INCB-054329; INCB-54329; 7-(3,5-Dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one. CAS No. 1628607-64-6. Molecular formula: C19H16N4O3. Mole weight: 348.36. | |
| INCB057643 | INCB057643 is a bromodomain and extraterminal domain (BET) inhibitor. It binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones. Synonyms: INCB-057643; 2,2,4-trimethyl-8-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-6-(methylsulfonyl)-2H-benzo[b][1,4]oxazin-3(4H)-one. CAS No. 1820889-23-3. Molecular formula: C20H21N3O5S. Mole weight: 415.46. | |
| Isoxazole | Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor? [1] [2] [3] [4] [5]. Uses: Scientific research. Group: Signaling pathways. CAS No. 288-14-2. Pack Sizes: 10 mM * 1 mL; 25 g; 50 g. Product ID: HY-W010649. | |
| (+)-JQ-1 | BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. Group: Biochemicals. Alternative Names: (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic Acid 1,1-Dimethylethyl Ester; (+)-JQ1; (S)-(+)-Tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate. Grades: Highly Purified. CAS No. 1268524-70-4. Pack Sizes: 5mg, 10mg, 25mg, 50mg, 100mg. Molecular Formula: C??H??ClN?O?S, Molecular Weight: 456.99. US Biological Life Sciences. | Worldwide |
| (+)-JQ-1 | (+)-JQ-1 is a potent and selective BET bromodomain inhibitor, IC50 values are 77 nM and 33 nM for inhibiting BRD4 (N-terminal) and BRD4 (C-terminal), respectively. Synonyms: JQ1. CAS No. 1268524-70-4. Molecular formula: C23H25ClN4O2S. Mole weight: 456.99. | |
| (+)-JQ-1 | (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))[1]. (+)-JQ-1 also activates autophagy[2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: JQ1. CAS No. 1268524-70-4. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 50 mg; 100 mg; 500 mg. Product ID: HY-13030. | |
| (+)-JQ1 carboxylic acid | (+)-JQ1 carboxylic acid is the carboxylic acid form of BET bromodomain inhibitor (+)-JQ1. Synonyms: JQ-1 carboxylic acid; (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetic acid. Grades: ≥98%. CAS No. 202592-23-2. Molecular formula: C19H17ClN4O2S. Mole weight: 400.881. | |
| JQ-1 (carboxylic acid) | JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4. Uses: Scientific research. Group: Signaling pathways. CAS No. 202592-23-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg. Product ID: HY-78695. | |
| (+)-JQ1 PA | (+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM. (+)-JQ1 PA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Uses: Scientific research. Group: Signaling pathways. CAS No. 2115701-93-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112789. | |
| Mivebresib | Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a K i of 1.5 nM [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ABBV-075. CAS No. 1445993-26-9. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-100015. | |
| Molibresib | Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC 50 of 32.5-42.5 nM. Uses: Scientific research. Group: Signaling pathways. Alternative Names: I-BET762; GSK525762; GSK525762A. CAS No. 1260907-17-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-13032. | |
| NEO2734 | NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains[1]. NEO2734 is active in SPOP mutant and wild-type prostate cancer[2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: EP31670. CAS No. 2081072-29-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136938. | |
| NVS-CECR2-1 | NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 ( CECR2 ) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity ( IC 50 =47 nM; K D =80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1992047-61-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-110374. | |
| ODM-207 | ODM-207 (BET-IN-4) is a potent BET bromodomain protein ( BRD4 ) inhibitor, with an IC 50 of ≤ 1 μM [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BET-IN-4. CAS No. 1801503-93-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-111916. | |
| Olinone | Olinone, a pyridoindol derivative, has been found to be an BET Bromodomain inhibitor and could be probably useful in sorts of biological studies. Synonyms: Olinone; SCHEMBL16771423; N-[4-(1-Oxo-1,2,3,4-Tetrahydro-5h-Pyrido[4,3-B]indol-5-Yl)butyl]acetamide. Grades: 98%. CAS No. 1770789-37-1. Molecular formula: C17H21N3O2. Mole weight: 299.37. | |
| OTX015 | OTX015 is a potent BET bromodomian inhibitor, which targets the BET bromodomain proteins 2, 3, and 4 (BRD). BRDs 2, 3, and 4 are considered potential cancer targets because of their pivotal role in regulating the transcription of growth-promoting genes and cell cycle regulators. Synonyms: OTX-015; OTX 015; MK-8628; MK 8628; MK8628; Birabresib; (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide. Grades: >98%. CAS No. 202590-98-5. Molecular formula: C25H22ClN5O2S. Mole weight: 492.00. | |
| PFI-1 | PFI-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs with acetylated histone tails. Co-crystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts. Intriguingly, cells exposed to PFI-1 showed significant down-regulation of Aurora B kinase, thus attenuating phosphorylation of the Aurora substrate H3S10 providing an alternative strategy for the specific inhibition of this well established oncology target. Synonyms: PFI1; PFI 1; PFI-1. CAS No. 1403764-72-6. Molecular formula: C16H17N3O4S. Mole weight: 347.39. | |
| PFI-1 | PFI-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs with acetylated histone tails. Co-crystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts. Uses: Designed for use in research and industrial production. Additional or Alternative Names: PFI1; PFI 1; PFI-1. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1403764-72-6. Molecular formula: C16H17N3O4S. Mole weight: 347.39. Purity: >98%. IUPACName: 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide. Canonical SMILES: O=S(C1=CC=CC=C1OC)(NC2=CC3=C(NC(N(C)C3)=O)C=C2)=O. Product ID: ACM1403764726. Alfa Chemistry ISO 9001:2015 Certified. Categories: PFM-1 mine. | |
| PLX51107 | PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range). Uses: Scientific research. Group: Signaling pathways. CAS No. 1627929-55-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-111422. | |
| PLX51107 | PLX51107 is a potent and selective BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2). It blocks the interaction mediated by the four BET family proteins. Synonyms: (S)-4-(6-(3,5-dimethylisoxazol-4-yl)-1-(1-(pyridin-2-yl)ethyl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid; PLX 51107; PLX-51107. CAS No. 1627929-55-8. Molecular formula: C26H22N4O3. Mole weight: 438.48. | |
| PPI Inhibitor Library | A unique collection of 260 PPI-related compounds for drug screening; - Targets include PD-1/PD-L1, Bcl-2, BET bromodomain, BRD4 bromodomain, etc. - Detailed compound information with structure, target, and biological activity description; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L9400. Categories: PPI Inhibitor Libraries. |  |
| (R)-(-)-JQ1 | (R)-(-)-JQ1 is the R-isomer and an inactive control of JQ1, a BET bromodomain inhibitor. Synonyms: (-)-JQ1; (-)-JQ 1; (-)-JQ-1; (R)-JQ1; (R)-(-)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate. Grades: >95%. CAS No. 1268524-71-5. Molecular formula: C23H25ClN4O2S. Mole weight: 456.989. | |
| RVX-208 | RVX-208 is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. Using binding assays and X-ray crystallography, we now show that RVX-208 selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. siRNA experiments further suggest that induction of ApoA-I mRNA is mediated by BET family member BRD4. These data indicate that RVX-208 increases ApoA-I production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis. Synonyms: RVX208; RVX 208; RVX-208; Apabetalone. Grades: >98%. CAS No. 1044870-39-4. Molecular formula: C20H22N2O5. Mole weight: 370.40. | |
| RVX297 | RVX297 is a BD2 selective inhibitor of BET bromodomains. It is structurally related to the clinical compound RVX-208. It has significant implications on differential gene expression, which possibly can be further linked to the specific disease indication. It is currently undergoing phase III clinical trials for the treatment of cardiovascular diseases. Uses: Rvx297 is used for the treatment of cardiovascular diseases. Synonyms: RVX-297; RVX 297; RVX297. 2-(3,5-Dimethyl-4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-5,7-dimethoxyquinazolin-4(3H)-one. Grades: >98 %. CAS No. 1044871-04-6. Molecular formula: C24H29N3O4. Mole weight: 423.51. | |
| RVX-297 | RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 ?M for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1044871-04-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-114504. | |
| Trotabresib | Trotabresib is a reversible inhibitor of epigenetic target bromodomain and extra-terminal (BET) protein with anti-tumor activity. Synonyms: CC 90010; CC-90010. Grades: >98%. CAS No. 1706738-98-8. Molecular formula: C21H21NO4S. Mole weight: 383.5. | |
| UMB-32 | UMB-32 is an inhibitor of the BET bromodomain BRD4 (Kd = 550 nM; IC50 = 637 nM) and the bromodomain-containing transcription factor TAF1 (Kd = 560 nM) and TAF1L (Kd = 1.3 μM). Synonyms: N-Tert-Butyl-2-[4-(3,5-Dimethyl-1,2-Oxazol-4-Yl)phenyl]imidazo[1,2-A]pyrazin-3-Amine. Grades: ≥98%. CAS No. 1635437-39-6. Molecular formula: C21H23N5O. Mole weight: 361.4. | |
| XD 14 | XD 14 is a BET bromodomain inhibitor (Kd = 160, 170, 380, 490, 830 and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2) respectively). XD 14 also inhibits BRDT(1), CBP, p300 and BRDT(2) (Kd = 1.2, 1.6, 2.6 and 3.7 μM, respectively). XD 14 inhibits proliferation of HL-60 leukemia cells in vitro. Synonyms: XD14; XD 14; XD-14; 4-Acetyl-N-[5-[(diethylamino)sulfonyl]-2-hydroxyphenyl]-3-ethyl-5-methyl-1H-pyrrole-2-carboxamide. Grades: ≥98% by HPLC. CAS No. 1370888-71-3. Molecular formula: C20H27N3O5S. Mole weight: 421.51. | |
| JQ1 Enantiomers Set ((S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate, SGCBD01, BRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I) | A cell-permeable I-BET class of thienodiazepine derivative whose (S)-(+), but not (R)-(-), enantiomer is shown to target both bromodomains (BD1 & BD2) of BET family members BRD2, BRD3, BRD4, and BRD6/BRDT in a Kac- (epsilon-N-acetylated lysine) competitive manner, exhibiting little affinity toward 23 other BD-containing proteins, BRD1 and BRD9, and little or no activity against a panel of more than 50 receptors, ion channels, and transporters. Effectively inhibits the oncogenic BRD4-NUT fusion-dependent NUT midline carcinoma and c-Myc oncoprotein-dependent multiple myeloma proliferation both in cultures (IC50 <1uM) in vitro and in mice (50mg/kg/day i.p.) in vivo. Also reported to cross the blood-testis boundary in male mice and effectively block BRDT-mediated spermatogenesis without affecting hormone levels. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1set. US Biological Life Sciences. | Worldwide |
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