UNC0379, Lysine Methyltransferase SETD8 Inhibitor


Catalog No. size PriceQuantity
M60207-2S 2 mg solid $129
M60207-10S 10mg solid $516

Description

UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. UNC0379 is active in multiple biochemical assays. Its affinity to SETD8 was confirmed by ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) studies. Importantly, UNC0379 is selective for SETD8 over 15 other methyltransferases. The lysine methyltransferase SETD8 is the only known methyltransferase that catalyzes monomethylation of histone H4 lysine 20 (H4K20). Monomethylation of H4K20 has been implicated in regulating diverse biological processes including the DNA damage response.

Product information

CAS Number: 1620401-82-2

Molecular Weight: 413.56

Formula: C23H35N5O2

Chemical Name: 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine

Smiles: COC1=CC2=C(NCCCCCN3CCCC3)N=C(N=C2C=C1OC)N1CCCC1

InChiKey: WEXCGGWTIDNVNT-UHFFFAOYSA-N

InChi: InChI=1S/C23H35N5O2/c1-29-20-16-18-19(17-21(20)30-2)25-23(28-14-8-9-15-28)26-22(18)24-10-4-3-5-11-27-12-6-7-13-27/h16-17H,3-15H2,1-2H3,(H,24,25,26)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

UNC0379 was used at 10-30 µM in vitro assays.

References:

  1. Ma A, et al. Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. (2014) J Med Chem. 57(15):6822-33.

Products are for research use only. Not for human use.

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