UNC0638 | 1933

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.

1933 | UNC0638 DataSheet

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