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。

27项目(s)

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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

27项目(s)

总面积,总面积
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