Bromodomain
Bromodomain(溴域)
Bromodomains are a family of evolutionarily conserved protein modules of approximately 110 amino acids that have been found in chromatin-associated proteins as well as nuclear histone acetyltransferases (HATs). Besides its role in chromatin remodeling, recent studies have identified that bromodomains, as acetyl-lysine binding domains, are able to recognize and bind ε–N-acetylated lysine residues in histone and non-histone proteins. The nuclear magnetic resonance (NMR) spectroscopic analysis reveals that the chemical structure of bromodomains, consisting of four left-handed α-helices (including αZ, αA, αB and αC) connected by two loops (ZA and BC loops), forms a deep hydrophobic cavity serving as the acetyl-lysine recognition site.
Bromodomain 相关产品(45)
- GC45640TP-238 (hydrochloride)CAS: 2415263-05-5纯度: >99.00%
A chemical probe for the bromodomains of CECR2 and BPTF
- GC10524GSK 525768ACAS: 1260530-25-3纯度: >99.00%
GSK 525768A 是 GSK525762A 的非活性对映异构体。 GSK 525768A 对 BET 没有任何活动。
- GC17973OTX-015CAS: 202590-98-5纯度: >99.50%
OTX-015 以浓度依赖性方式抑制 BRD2、BRD3 和 BRD4 与乙酰化组蛋白 4 的结合，IC50 值为 92-112nM .OTX-015 在九个 AML 细胞系中的六个和所有四个 ALL 细胞系中测量到显着的生长抑制:HEL IC50 值为 248 nM，NB4 IC50值为 233 nM，NOMO-1 IC50 值为 229 nM，KG1 IC50 值为 198 nM，OCI-AML3 IC50 值为Kasumi IC50 值为 60 nM，Kasumi IC50 值为 17 nM，JURKAT IC50 值为 249 nM，BV-173 IC50 值为 161 nM , TOM-1 IC50 值为 133 nM, RS4-11 IC50 值为 34 nM。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC43320 | CPI-268456 | 1380087-86-4 | >98.00% | |
A ligand of BRD4 | ||||
| GC43889 | I-CBP112 (hydrochloride) | 2147701-33-3 | >90.00% | |
A p300 and CBP inhibitor | ||||
| GC45503 | L-Moses (hydrochloride) | - | >98.00% | |
A PCAF bromodomain inhibitor | ||||
| GC45640 | TP-238 (hydrochloride) | 2415263-05-5 | >99.00% | |
A chemical probe for the bromodomains of CECR2 and BPTF | ||||
| GC46675 | 4-Phenyl-2-pyrrolidinone | 1198-97-6 | >98.00% | |
A precursor and synthetic intermediate | ||||
| GC48408 | TW9 | 2614417-90-0 | >98.00% | |
A dual inhibitor of BRD4 and HDAC1 | ||||
| GC49029 | CAY17c | 2414373-11-6 | >98.00% | |
An inhibitor of BRD4 and class I and class IIb HDACs | ||||
| GC50070 | I-BET 151 dihydrochloride | 1883545-47-8 | - | |
A BRD2, BRD3, and BRD4 inhibitor | ||||
| GC60182 | GSK046 | 2474876-09-8 | >98.00% | |
A BD2 bromodomain inhibitor | ||||
| GC10402 | Bromosporine | 1619994-69-2 | >99.50% | |
A non-specific bromodomain inhibitor | ||||
| GC10524 | GSK 525768A | 1260530-25-3 | >99.00% | |
GSK 525768A 是 GSK525762A 的非活性对映异构体。 GSK 525768A 对 BET 没有任何活动。 | ||||
| GC14199 | RVX-208 | 1044870-39-4 | >99.00% | |
A selective BET bromodomain antagonist | ||||
| GC15375 | PFI-1 (PF-6405761) | 1403764-72-6 | >99.50% | |
A BET bromodomain inhibitor | ||||
| GC15747 | I-BET151 (GSK1210151A) | 1300031-49-5 | >99.50% | |
A BRD2, BRD3, and BRD4 inhibitor | ||||
| GC16794 | UNC1215 | 1415800-43-9 | >98.00% | |
Potent L3MBTL3 domain inhibitor | ||||
| GC17073 | I-BET-762 | 1260907-17-2 | >99.00% | |
Inhibitor of BET proteins | ||||
| GC17973 | OTX-015 | 202590-98-5 | >99.50% | |
OTX-015 以浓度依赖性方式抑制 BRD2、BRD3 和 BRD4 与乙酰化组蛋白 4 的结合，IC50 值为 92-112nM .OTX-015 在九个 AML 细胞系中的六个和所有四个 ALL 细胞系中测量到显着的生长抑制:HEL IC50 值为 248 nM，NB4 IC50值为 233 nM，NOMO-1 IC50 值为 229 nM，KG1 IC50 值为 198 nM，OCI-AML3 IC50 值为Kasumi IC50 值为 60 nM，Kasumi IC50 值为 17 nM，JURKAT IC50 值为 249 nM，BV-173 IC50 值为 161 nM , TOM-1 IC50 值为 133 nM, RS4-11 IC50 值为 34 nM。 | ||||
| GC18096 | UNC669 | 1314241-44-5 | >98.50% | |
A selective MBT inhibitor | ||||
| GC13148 | MS436 | 1395084-25-9 | >99.00% | |
MS436 是一类新的溴结构域抑制剂，对 BRD4 BrD1 具有估计的 Ki=30-50 nM 的强亲和力，对 BrD2 的选择性是 10 倍。 | ||||
| GC14063 | GSK1324726A | 1300031-52-0 | >98.00% | |
A selective inhibitor of BET family proteins | ||||
| GC14699 | CPI-203 | 1446144-04-2 | >99.00% | |
A bioavailable inhibitor of BET bromodomains | ||||