GSK-3484862 | CAS#2170136-65-7 | Dnmt1 inhibitor

MedKoo Cat#: 462425 | Name: GSK-3484862

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK-3484862 is a non-covalent inhibitor for Dnmt1. GSK-3484862 induces DNA hypomethylation to against cancer.

Chemical Structure

GSK-3484862

CAS#2170136-65-7

Theoretical Analysis

MedKoo Cat#: 462425

Name: GSK-3484862

CAS#: 2170136-65-7

Chemical Formula: C19H19N5OS

Exact Mass: 365.1310

Molecular Weight: 365.46

Elemental Analysis: C, 62.45; H, 5.24; N, 19.16; O, 4.38; S, 8.77

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 Weeks
10mg	USD 600.00	2 Weeks

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Related CAS #

No Data

Synonym

GSK-3484862; GSK3484862; GSK 3484862; GSKMI-714; GSKMI714; GSKMI 714; NSC-825088; NSC825088; NSC 825088

IUPAC/Chemical Name

(R)-2-((3,5-dicyano-6-(dimethylamino)-4-ethylpyridin-2-yl)thio)-2-phenylacetamide

InChi Key

KIEQQZZDWUNUQK-MRXNPFEDSA-N

InChi Code

InChI=1S/C19H19N5OS/c1-4-13-14(10-20)18(24(2)3)23-19(15(13)11-21)26-16(17(22)25)12-8-6-5-7-9-12/h5-9,16H,4H2,1-3H3,(H2,22,25)/t16-/m1/s1

SMILES Code

O=C(N)[C@H](SC1=NC(N(C)C)=C(C#N)C(CC)=C1C#N)C2=CC=CC=C2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

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 Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer.

In vitro activity:

In total, methylation mapping supports the conclusion that GSK-3484862 treatment produces a drop in DNA methylation consistent with selective and near complete inhibition of DNMT1. Reference: Epigenetics Chromatin. 2021 Dec 15;14(1):56. https://pubmed.ncbi.nlm.nih.gov/34906184/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	20.8	57.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 365.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Azevedo Portilho N, Saini D, Hossain I, Sirois J, Moraes C, Pastor WA. The DNMT1 inhibitor GSK-3484862 mediates global demethylation in murine embryonic stem cells. Epigenetics Chromatin. 2021 Dec 15;14(1):56. doi: 10.1186/s13072-021-00429-0. PMID: 34906184; PMCID: PMC8672470.

In vitro protocol:

In vivo protocol:

TBD

1: Keystone Symposia 2019 - Epigenetics and Human Disease