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I-138 是一种具有口服活性和有效性的 USP1-UAF1 可逆抑制剂。I-138 促使细胞中 FANCD2 和 PCNA 的单泛素化,抑制细胞中的 USP1 自裂解。
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I-138 是一种具有口服活性和有效性的 USP1-UAF1 可逆抑制剂。I-138 促使细胞中 FANCD2 和 PCNA 的单泛素化,抑制细胞中的 USP1 自裂解。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,870 | 现货 | |
5 mg | ¥ 3,230 | 现货 | |
10 mg | ¥ 4,620 | 现货 | |
25 mg | ¥ 7,120 | 现货 | |
50 mg | ¥ 9,590 | 现货 | |
100 mg | ¥ 12,900 | 现货 | |
200 mg | ¥ 17,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 3,550 | 现货 |
产品描述 | I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells. |
体外活性 | I-138 (0.5 μM; 4 hours) eliminates HAP-1 USP1 WT and knockout cells' USP1 autodeubiquitination[1]. I-138 (0.5 μM; 4 hours) induces monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells[1].I-138 (0.01-10 μM; 10 days) dose-dependently inhibits the viability of MDA-MB-436 cells without affecting HCC1954 cells[1]. |
体内活性 | I-138 (50 mg/kg/day; oral administration; for 41 days) exhibits USP1 inhibition and moderate antitumor activity in mice carrying MDA-MB-436 tumors. However, the combination of I-138 and the PARP inhibitor Niraparib is more effective in inhibiting BRCA1/2 mutant tumors in vivo[1]. |
分子量 | 492.5 |
分子式 | C26H23F3N6O |
CAS No. | 2098211-50-6 |
存储 | store at low temperature,keep away from direct sunlight | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 80 mg/mL (162.44 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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