Description
Cell-permeable. UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC₅₀ value of <15 nM in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC₅₀ value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC₅₀ value of 81 nM and demonstrates favorable separation of functional and toxic effect.
UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC₅₀ value of <15 nM in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC₅₀ value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC₅₀ value of 81 nM and demonstrates favorable separation of functional and toxic effect.
Alternate Name/Synonyms: 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Appearance: Off-white solid
Formulation: N/A
CAS Number: 1255580-76-7
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₃₀H₄₇N₅O₂
Molecular Weight: 509.72
Cell-Permeable?: Yes
Purity: ≥98% by HPLC
Solubilities: DMSO (10 mM)
Handling: Protect from air and light
Country of Origin: USA
Tag Line: Apotent G9a HMTase inhibitor
MDL Number: MFCD17215972
PubChem CID: 46224516
SMILES: CC(C)N1CCC(CC1)NC2=NC(=NC3=CC(=C(C=C32)OC)OCCCN4CCCC4)C5CCCCC5
InChi: InChI=1S/C30H47N5O2/c1-22(2)35-17-12-24(13-18-35)31-30-25-20-27(36-3)28(37-19-9-16-34-14-7-8-15-34)21-26(25)32-29(33-30)23-10-5-4-6-11-23/h20-24H,4-19H2,1-3H3,(H,31,32,33)
InChi Key: QOECJCJVIMVJGX-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |