ML-323|ML323|USP1-UAF1 inhibitor

Cas No.:	1572414-83-5
Chemical Name:	ML323; ML 323
Synonyms:	ML323; ML 323
SMILES:	C(C1=CC=CC=C1C(C)C)1=NC=C(C)C(NCC2=CC=C(N3C=CN=N3)C=C2)=N1
Formula:	C₂₃H₂₄N₆
M.Wt:	384.48
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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.

In Vitro:

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[1]. 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[2].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC8319	Spautin 1	Spautin 1 is an inhibitor of autophagy; inhibits USP10 and USP13 activity (IC50 values are 0.6 and 0.7 μM respectively) and promotes degradation of Vps34 (class III PI 3-kinase) complexes.
DC10001	NSC632839	NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.
DC10091	ML364	ML364 is an USP2 inhibitor.xtracted from patent WO 2016134026 A1, compound example 10G.
DC7468	ML-323	ML323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a 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.
DC7610	LDN-57444	LDN-57444 is a reversible, competitive proteasome inhibitor for Uch-L1 with IC50 of 0.88 μM, 28-fold selectivity over isoform Uch-L3.
DC12495	GNE-6640	GNE-6640 is a potent, selective USP7 inhibitor with IC50 of 0.75 uM; dislpalys selectivity over USP47 and USP5 (IC50>200 uM).
DC10838	F1063-0967	F1063-0967 is a Dual-specificity phosphatase 26 (DUSP26) inhibitor with an IC50 of 11.62 μM.