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].
Product Specifications
CAS Number
2170137-61-6
UNSPSC
12352005
Target
DNA Methyltransferase
Type
Reference compound
Related Pathways
Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/gsk-3685032.html
Purity
99.95
Solubility
DMSO : 25 mg/mL (ultrasonic)
Smiles
N#CC1=C(SC(C2=CC=CC=C2)C(N)=O)N=C(N3CCC(CC3)N)C(C#N)=C1CC
Molecular Formula
C22H24N6OS
Molecular Weight
420.53
References & Citations
[1]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
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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