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.
Products for Bromodomain
- 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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GC48408
TW9
A dual inhibitor of BRD4 and HDAC1
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GC46675
4-Phenyl-2-pyrrolidinone
4-苯基-2-吡咯烷酮
A precursor and synthetic intermediate -
GC18750
NEO2734
EP31670
NEO2734 (EP31670) 是一种口服有效的双重 p300/CBP 和 BET 溴结构域选择性抑制剂,对 p300/CBP 和 BET 溴结构域的 IC50 值均 <30 nM。 NEO2734 在 SPOP 突变型和野生型前列腺癌中具有活性。 -
GC60182
GSK046
iBET-BD2
A BD2 bromodomain inhibitor -
GC50070
I-BET 151 dihydrochloride
GSK1210151A dihydrochloride
A BRD2, BRD3, and BRD4 inhibitor -
GC45640
TP-238 (hydrochloride)
A chemical probe for the bromodomains of CECR2 and BPTF
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GC45503
L-Moses (hydrochloride)
L-45
A PCAF bromodomain inhibitor -
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抑制剂,CPI-0610; CPI0610; CPI 0610
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。 -
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
(2E)-1-(2-羟基苯基)-3-[(1R,4R)-5-(2-吡啶基)-2,5-二氮杂双环[2.2.1]庚-2-基]-2-丙烯-1-酮
Probe for bromodomains of SMARCA2/4 and PB1(bromodomain 5) -
GC14699
CPI-203
A bioavailable inhibitor of BET bromodomains
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GC14063
GSK1324726A
I-BET726
A selective inhibitor of BET family proteins -
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)
7-(3,5-二甲基异噁唑-4-基)-8-甲氧基-1-((R)-1-(吡啶-2-基)乙基)-1H-咪唑并[4,5-C]喹啉-2(3H)-酮,GSK1210151A
A BRD2, BRD3, and BRD4 inhibitor -
GC17073
I-BET-762
(4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-A][1,4]苯并二氮杂卓-4-乙酰胺,I-BET762; GSK525762; GSK525762A
Inhibitor of BET proteins -
GC14199
RVX-208
阿帕他隆; RVX-208; RVX000222
A selective BET bromodomain antagonist -
GC18096
UNC669
A selective MBT inhibitor
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GC10174
SGC-CBP30
SGCCBP30,SGC CBP30
A potent inhibitor of CREBBP/EP300 bromodomains -
GC16794
UNC1215
UNC 1215;UNC-1215
Potent L3MBTL3 domain inhibitor -
GC17973
OTX-015
OTX 015;OTX015
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。 -
GC10524
GSK 525768A
GSK525768A;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。 -
GC10402
Bromosporine
A non-specific bromodomain inhibitor
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GC15375
PFI-1 (PF-6405761)
PF06405761
A BET bromodomain inhibitor -
GC13822
(-)-JQ1
(S)-(+)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂卓-6-基)乙酸叔丁酯,(-)-JQ1
A selective inhibitor of BET bromodomains -
GC16531
Bromodomain Inhibitor, (+)-JQ1
(S)-(+)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂卓-6-基)乙酸叔丁酯
A selective inhibitor of BET bromodomains