产品名称

英文名称：SJB2-043

同义词

sjb2-043、63388-44-3、2-PHENYLNAPHTHO[2,3-D]OXAZOLE-4,9-DIONE、2-phenylbenzo[f][1,3]benzoxazole-4,9-dione、CHEMBL3407552、SJB2 043、2-Phenyl-naphth[2,3-d]oxazole-4,9-dione、2-phenyl-naphtho[2,3-d]oxazole-4,9-dione、SCHEMBL7808226、GTPL12225、DTXSID40333501、SJB2043

产品性质

CAS编号：63388-44-3

分子式：C17H9NO3

分子量：275.26

PubChem编号：509070

英文别名：sjb2-043|63388-44-3|2-PHENYLNAPHTHO[2,3-D]OXAZOLE-4,9-DIONE|2-phenylbenzo[f][1,3]benzoxazole-4,9-dione|CHEMBL3407552|SJB2 043|2-Phenyl-naphth[2,3-d]oxazole-4,9-dione|2-phenyl-naphtho[2,3-d]oxazole-4,9-dione|SCHEMBL7808226|GTPL12225|DTXSID40333501|SJB2043|

规格或纯度：98%

英文名称：SJB2-043

生化机理：IC50 Value 0.544 uM (USP1) SJB2-043 is one of analogs/derivatives of C527, which is a novel and potent USP1 (ubiquitin-specific protease 1) inhibitor. Cells were treated with SJB2-043 for 24 hrs and cell extracts were incubated with HA-Ub-VS, followed by immunoblotting with anti-USP1 or anti-HA antibodies. Consistent with our previous studies and the most recent studies by Piatkov et al (24, 31, 33), USP1 in the untreated cells was detected on western blot as a doublet; full length USP1 and an auto-cleaved USP1 with only N-terminus. The Ub-USP1 conjugates were generated in the untreated cell lysates and were detected by an increase in molecular weight of USP1. However, the formation of the Ub-USP1 conjugate was inhibited by the addition of SJB2-043. Ub-aldehyde, a potent known nonspecific DUB inhibitor, caused a complete loss of USP1-Ub-VS conjugates in this competition assay.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍 SJB2-043 抑制 USP1/UAF1 复合体，IC50 为 544 nM。 SJB2-043是一种新型有效的USP1抑制剂，IC50值为0.544 μM。 泛素特异性蛋白酶1（USP1）是一种去泛素化酶（DUB），是泛素特异性加工（UBP）蛋白酶家族的成员。USP1去泛素化Fanconi贫血症（FA）DNA修复途径中的一个蛋白。 在K562细胞中，SJB2-043以剂量依赖的方式减少USP1水平，通过蛋白酶体降解途径引起ID1蛋白的降解。SJB2-043也减少ID2和ID3蛋白的水平。重要的是，USP1敲除可抑制细胞生长，增加细胞凋亡。在原代AML细胞中，SJB2-043灭活USP1，促进ID1降解。在原代人脐血CD34+细胞中，SJB2-043在低微摩尔水平时抑制细胞生长。在HeLa细胞中，SJB2-043增加Ub-FANCD2和Ub-PCNA的水平。FANCD2的去泛素化是BRCA/Fanconi贫血症（FA）DNA修复途径中的重要步骤。

IUPAC Name：2-phenylbenzo[f][1,3]benzoxazole-4,9-dione

INCHI：InChI=1S/C17H9NO3/c19-14-11-8-4-5-9-12(11)15(20)16-13(14)18-17(21-16)10-6-2-1-3-7-10/h1-9H

InChi Key：CMYQQADDUUDCCA-UHFFFAOYSA-N

Canonical SMILES：C1=CC=C(C=C1)C2=NC3=C(O2)C(=O)C4=CC=CC=C4C3=O

Isomeric SMILES：C1=CC=C(C=C1)C2=NC3=C(O2)C(=O)C4=CC=CC=C4C3=O

PubChem CID：509070

ChEMBL Ligand：CHEMBL3407552

CAS Registry No.：63388-44-3

溶解性：insoluble in H2O; insoluble in EtOH; ≥6.68 mg/mL in DMSO

产品包装