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.
- Cat.No. 产品名称 Information
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GC49029
CAY17c
An inhibitor of BRD4 and class I and class IIb HDACs
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GC48548
iBET-BD2
A BD2 bromodomain inhibitor
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GC48408
TW9
A dual inhibitor of BRD4 and HDAC1
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GC46675
4-Phenyl-2-pyrrolidinone
A precursor and synthetic intermediate
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GC50070
I-BET 151 dihydrochloride
A BRD2, BRD3, and BRD4 inhibitor
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GC43889
I-CBP112 (hydrochloride)
A p300 and CBP inhibitor
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GC43320
CPI-268456
A ligand of BRD4
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GC14168
UMB-32
An inhibitor of BRD4, TAF1, and TAF1L bromodomains
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GC16763
NI-57
A BRPF bromodomain inhibitor
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GC13025
GSK6853
A selective chemical probe for the bromodomain of BRPF1
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GC13014
AZD 5153
A BRD4 inhibitor
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GC10382
CPI-637
An inhibitor of CBP/EP300 bromodomains
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GC15152
PF-CBP1
An inhibitor of the CBP and p300 bromodomains
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GC16726
BI-7273
A potent BRD9 bromodomain inhibitor
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GC16817
BI-9564
A selective BRD9/7 bromodomain inhibitor
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GC12588
I-BRD9
A BRD9 bromodomain inhibitor
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GC15789
GSK2801
A probe for BAZ2A/B bromodomains
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GC10979
PFI 4
A chemical probe for BRPF1
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GC16299
BET bromodomain inhibitor
BET 溴结构域抑制剂是从专利 WO/2015/153871A2 化合物实施例 11 中提取的一种有效的 BET 抑制剂。
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GC14655
OXF BD 02
OXF BD 02 是 BRD4(1)(BRD4 的第一个溴结构域)的选择性抑制剂,IC50 值为 382 nM。
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GC10727
Ischemin sodium salt
CBP bromodomain inhibitor
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GC12440
GSK 5959
An inhibitor of the BRPF1 bromodomain
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GC15175
BAZ2-ICR
A BAZ2A/B bromodomain inhibitor
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GC17482
OF-1
A bromodomain probe for BRPF proteins
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GC16611
GW841819X
BET bromodomain inhibitor
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GC13187
I-BET 151 hydrochloride
A BRD2, BRD3, and BRD4 inhibitor
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GC14361
PFI 3
Probe for bromodomains of SMARCA2/4 and PB1(bromodomain 5)
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GC14699
CPI-203
A bioavailable inhibitor of BET bromodomains
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GC14063
GSK1324726A
A selective inhibitor of BET family proteins
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GC13148
MS436
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。
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GC15747
I-BET151 (GSK1210151A)
A BRD2, BRD3, and BRD4 inhibitor
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GC17073
I-BET-762
Inhibitor of BET proteins
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GC14199
RVX-208
A selective BET bromodomain antagonist
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GC18096
UNC669
A selective MBT inhibitor
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GC10174
SGC-CBP30
A potent inhibitor of CREBBP/EP300 bromodomains
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GC17944
I-CBP 112
A p300 and CBP inhibitor
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GC16794
UNC1215
Potent L3MBTL3 domain inhibitor
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GC17973
OTX-015
A BRD2, BRD3, and BRD4 inhibitor
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GC10524
GSK 525768A
GSK 525768A 是 GSK525762A 的非活性对映异构体。 GSK 525768A 对 BET 没有任何活动。
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GC10402
Bromosporine
A non-specific bromodomain inhibitor
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GC15375
PFI-1 (PF-6405761)
A BET bromodomain inhibitor
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GC13822
(-)-JQ1
A selective inhibitor of BET bromodomains
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GC16531
Bromodomain Inhibitor, (+)-JQ1
A selective inhibitor of BET bromodomains