Acetylated Lysine
BRPFs(bromodomain and PHD finger-containing proteins)are multidomain proteins of the Trithorax group(TrxG):regulatory proteins composed of diverse,evolutionary conserved units that form chromatin-associated complexes accounting for电子传输量.Three BRPFs are known to date,sharing>65%homology in their~100amino acid counting sequences,all sharing an acetylated lysine(KAc)recognition site that closely resembles other bromodomains,including those of theBETs[1].BRPF1(also known as Br140 and Peregrin)is a component of complexes containing the MOZ/MORF transcriptional coactivators,that links the catalytic HATs to the other subunits ING5and hEAF6.Furthermore,BRPF1contains PHD fingers,a bromodomain and a PWWP domain[2].It has been shown that BRPF1has a central role during development,since mutations have shown to display anterior transformations of pharyngeal arches due to progressive loss of anterior Hox gene expression.What’s more,translocations of MOZ are associated with aggressive subtypes of leukemia,and make BRPF1an interesting target in oncology related research[3]。
[1]E.H.Demont et al.1,3-Dimethyl Benzimidazolones Are Potent,Selective Inhibitors of the BRPF1Bromodomain.ACS Med Chem Lett.2014Sep10;5(11):1190-5。
[2]K.Laue et al.The multidomain protein Brpf1binds histones and is required for Hox gene expression and segmental identity.Development.2008Jun;135(11):1935-46。
[3]L.You et al.The chromatin regulator brp1regulates embryo development and cell proliferation.J Biol Chem.2015May1;290(18):11349-64。
Axon ID |
Name |
说明,说明 |
自打印,自打印 |
1989
|
(+)-JQ1
|
Potent and selective BET bromodomain inhibitor |
€60.00 |
3822
|
(+)-JQ1carboxylic acid
|
(+)-JQ1derivative;PROTAC precursor |
€110.00 |
3873
|
(-)-JQ-1
|
Inactive enantiomer of(+)-JQ1 |
€120.00 |
3696
|
ABBV-075
|
高性能和可操作BET bromodomain(BRD)inhibitor |
€110.00 |
3956
|
ABBV-744
|
First-in-class high ly BDI(Bromodomain II)-selective BET bromodomain inhibitor |
Inquire |
3944
|
ARV-825
|
Potent and selective protein BRD4 degrader |
Inquire |
3833
|
AZD5153HNT salt
|
Potent,selective,and orally available BET/BRD4 bromodomainhibitor |
Inquire |
3037
|
BI-894999
|
Potent,selective and orally active BET inhibitor |
€165.00 |
3716
|
BMS-986158
|
BET bromodomain(BRD)inhibitor |
Inquire |
3933
|
CCS-1477
|
Potent,selective and orally bioavailable inhibitor of the Bromodomain of p300and CBP |
Inquire |
2776
|
CD161
|
Potent,selective,and orally active BET bromodomain inhibitor |
€135.00 |
3764
|
CFT-8634
|
Selective orally bioavailable BRD9 degrader |
Inquire |
2594
|
CPI0610
|
选择和metabolically stable inhibitor of BET bromodomains |
Inquire |
3922
|
dveET1
|
BET bromodomain degrader |
Inquire |
3769
|
FHD-286
|
BRG1/BRM |
Inquire |
2410
|
GSK5959
|
BRPF1bromodomain |
€135.00 |
3921
|
GSK046
|
Domain-selective and orally active inhibitor of BET with immunomodulatory activity |
Inquire |
4135
|
I-BET 151
|
BET bromodomain inhibitor |
Inquire |
3860
|
I-BET 726
|
Potent and selective,tetrahydroquinoline-based small molecule ligand binding to BET proteins |
Inquire |
4134
|
I-BET762
|
BET bromodomain inhibitor |
Inquire |
3186
|
NVS-BPTF-1
|
Potent,selective and cell active chemical probe for BPTF |
€180.00 |
3329
|
ODM-207
|
Highly potent,selective and orally active pan-BET inhibitor |
€140.00 |
2442
|
OF-1
|
BRPF1和BRPF2 selective |
€80.00 |
2530
|
OTX015
|
BRD2、BRD3和BRD4 with clear anti-proliferative activity |
€110.00 |
1887
|
PFI-1
|
BET bromodomain(BRD)inhibitor |
€75.00 |
2245
|
RVX208
|
BET bromodomainhibitor specific for second bromodomains(BD2s) |
€65.00 |
3623
|
SGC-SMARCA-BRDVIII
|
Potent,highly selective and cell-active SMARCA2/4and PB1(5)bromodomain inhibitor |
€90.00 |