(R) -GSK-3685032

(R) -GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1][2].

Product Specifications

CAS Number

[2170140-50-6]

UNSPSC

12352005

Target

DNA Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/r-gsk-3685032.html

Purity

98.97

Solubility

DMSO : 60 mg/mL (ultrasonic)

Smiles

N#CC1=C(N2CCC(CC2)N)N=C(C(C#N)=C1CC)S[C@H](C3=CC=CC=C3)C(N)=O

Molecular Formula

C22H24N6OS

Molecular Weight

420.53

References & Citations

[1]Adams, Nicholas David, et al. Substituted pyridines as inhibitors of DNMT1 and their preparation. WO2017216727A1.|[2]Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2 (10) :1002-1017.