Home Ubiquitin DUB inhibitor ML323

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ML323 DUB inhibitor

Cat.No.S7529

ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM.
ML323 DUB inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 384.48

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Chemical Information, Storage & Stability

Molecular Weight 384.48 Formula

C23H24N6

 Storage (From the date of receipt)
CAS No. 1572414-83-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CN=C(N=C1NCC2=CC=C(C=C2)N3C=CN=N3)C4=CC=CC=C4C(C)C

Solubility

In vitro
Batch:

DMSO : 76 mg/mL ( (197.66 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 38 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features
USP1-UAF1-selective inhibitor.
Targets/IC50/Ki
USP1-UAF1 [1]
(Cell-free assay)
76 nM
In vitro

ML323 inhibits the deubiquitination of PCNA and FANCD2 by inhibiting USP1–UAF1 activity in H596 cells. Moreover, this compound potentiates cytotoxicity in NSCLC H596 cells and U2OS osteosarcoma cells by targeting two major DNA damage response pathways (TLS and FA). [1]
Kinase Assay
High-throughput screening
For HTS, USP1-UAF1 activity is monitored using ubiquitin-rhodamine 110 as a substrate. The assay is miniaturized to a 4 μL volume in a 1,536-well format and is used to screen approximately 402,701 compounds in quantitative HTS mode, with each compound tested over a range of four to five concentrations. The assay shows robust performance with an average Z’factor of 0.8 throughout the screen.
In vivo

This compound is a selective USP1–UAF1 inhibitor that inhibit deubiquitinase activity of USP1–UAF1 complex.
References

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