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: ≥12 months 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:
- 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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