(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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture and light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
DNMT1
Available Sizes
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