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抑制剂/激活剂

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凋亡与自噬

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ML-323

ML-323 是一种有效的可逆的 USP1-UAF1 抑制剂，在Ub-Rho实验中，IC50 为 76 nM。

货号：
TK0509
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	1572414-83-5
生物活性	ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
分子式	C23H24N6
分子量	384.48
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 49 mg/mL (127.44 mM)
体外研究	ML-323 (ML323) is a highly potent inhibitor of the USP1-UAF1 deubiquitinase complex with excellent selectivity against human DUBs, deSUMOylase, deneddylase and unrelated proteases. ML-323 is a potent USP1-UAF1 inhibitor with IC50 values of 76 nM in a ubiquitin-rhodamine (Ub-Rho) assay and 174 nM and 820 nM in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) and monoubiquitinated PCNA (Ub-PCNA) as substrates, respectively. ML-323 probably exerts its inhibitory effect through an allosteric mechanism. The measured inhibition constants of ML-323 for the free enzyme (Ki) and the enzyme-substrate complex (K’i) are 68 nM and 183 nM. Besides, ML-323 potentiates Cisplatin cytotoxicity in non-small cell lung cancer and osteosarcoma cells. ML-323 (ML323), a probe molecule that displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1. In addition, ML-323 potentiates the cytotoxicity of Cisplatin and increases endogenous monoubiquitination levels of both PCNA and FANCD2, two known cellular targets of USP1/UAF1.
文献	•EMBO J. 2015 May 12;34(10):1385-98. •Cell Chem Biol. 2021 Apr 27;S2451-9456(21)00213-0. •Cell Prolif. 2020 Oct;53(10):e12908. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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