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Sigma-Aldrich

Protein Lysine Methyltransferase Inhibitor, UNC0321

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Synonym(s):
Protein Lysine Methyltransferase Inhibitor, UNC0321, 7-(2-(2-(Dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Empirical Formula (Hill Notation):
C27H45N7O3
Molecular Weight:
515.69

Assay

>98% (HPLC)

Quality Level

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

light tan

solubility

DMSO: 100 mg/mL

shipped in

wet ice

storage temp.

−20°C

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This Item
382192124030371822
GPR120 Agonist III The GPR120 Agonist III controls the biological activity of GPR120. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

Sigma-Aldrich

371822

GPR120 Agonist III

form

solid

form

powder

form

solid

form

powder

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, protect from light

color

light tan

color

off-white

color

yellow

color

white

solubility

DMSO: 100 mg/mL

solubility

DMSO: 10 mg/mL

solubility

DMSO: 25 mg/mL, water: 50 mg/mL

solubility

DMSO: 100 mg/mL

General description

A cell-permeable quinazoline analog that potently and selectively inhibits PKMT G9a with IC50s equal to 6 µM and 9 µM in two biochemical assays (CLOT and ECSD respectively), and a Morrison Ki of 63 pM, which is about 250-fold more potent compared with a close analog BIX01294 (Cat. No. 382190). Also inhibited GLP with reduced potency (15 µM in an ECSD enzymatic assay). It was found to be inactive (IC50>40 µM) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3 in the ECSD assays as well as JMJD2E with >1000-fold selectivity.
A cell-permeable, quinazoline analog that potently and selectively inhibits PKMT G9a (IC50 = 6 nM and 9 nM in two biochemical assays for CLOT and ECSD, respectively, and Ki = 63 pM, which is approximately 250-fold more potent than a closely-related analog, BIX01294 (Cat. No. 382190)). It inhibits GLP with reduced potency (15 nM) and is found to be inactive (IC50 >40 µM) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3, as well as JMJD2E (>1000-fold selectivity) in ECSD enzymatic assays. It also inhibits H3K9me2 accumulation (IC50 = 11,000 nM) in MDA-MB-231 cells, in comparison to BIX01294 (IC50 = 500 nM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Liu, F., et al. 2010. J. Med. Chem.53, 5844.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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