GSK3685032 free base · Synonyms: GSK-3685032 · GSK 3685032

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor.

For research use only. Not for human or veterinary use.

Target DNA Methyltransferase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK3685032 structure

CAS No.: 2170137-61-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 587.00	BP-02228-100mg	In stock	Get quote
250 mg	USD 992.00	BP-02228-250mg	In stock	Get quote
500 mg	USD 1,248.00	BP-02228-500mg	In stock	Get quote
1 g	USD 1,842.00	BP-02228-1g	In stock	Get quote
5 g	Inquire	BP-02228-5g	In stock	Inquire
10 g	Inquire	BP-02228-10g	In stock	Inquire

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Description

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM.

Biological activity

GSK3685032, a potent first-in-class DNMT1-selective inhibitor that was shown via crystallographic studies to compete with the active-site loop of DNMT1 for penetration into hemi-methylated DNA between two CpG base pairs.

Identifiers

SMILES: N#CC1=C(SC(C2=CC=CC=C2)C(N)=O)N=C(N3CCC(CC3)N)C(C#N)=C1CC
InChIKey: KNKHRZYILDZLRE-UHFFFAOYSA-N

Specifications

MW (average): 420.5310
Formula: C₂₂H₂₄N₆OS
CAS No.: 2170137-61-6
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 25 mg/mL

Documents

References

[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.

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