UNC0379 trifluoroacetate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

UNC0379 是赖氨酸甲基转移酶 SETD8 的选择性 +N2106:AC2106 底物竞争性抑制剂，IC50 为 7.3 uM。

UNC0379 is a selective, +N2106:AC2106substrate-competitive inhibitor of lysine methyltransferase SETD8 with IC50 of 7.3 uM, displays good selectivity over 15 other methyltransferases, including G9a and GLP (IC50>100 uM); causes neuroblastoma (NB) cell growth inhibition which is p53 dependent, reduces levels of p53K382me1 modification in xenografts.

UNC0379 TFA (1-10 μM, 9 days) inhibits HGSOC cells proliferation.UNC0379 TFA (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells.UNC0379 TFA (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation. Cell Viability Assay Cell Line:JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu Concentration:1-10 μM Incubation Time:9 days Result:Inhibited HGSOC cells proliferation with IC50s ranging from 0.39 to 3.20 μM.Cell Cycle Analysis Cell Line:JHOS3, OVCAR3 Concentration:10 μM Incubation Time:96 h Result:Arrested cells in sub-G1 phase.

UNC0379 TFA (intratracheal administration, 1 mg/kg/day, 1 mg/kg/day, on day7, 8, and 9) ameliorates the lung fibrosis in Bleomycin (BLM)-induced lung fibrosis mouse. Animal Model:Bleomycin (BLM)-induced lung fibrosis mouse modelDosage:1 mg/kg/day Administration:Intratracheal administration, on day7, 8, and 9.Result:Ameliorated BLM-induced lung fibrosis (supported by the evaluation of the Ashcroft score and changes in the collagen content in the lung samples) without affecting pulmonary inflammation.

UNC-0379 trifluoroacetate

Chromatin/Epigenetic

HMTase

HMTase

Other Indications

——

1620401-83-3

527.5797

C25H36F3N5O4

>98% (HPLC)

10 mM in DMSO

COC1=CC2=NC(N3CCCC3)=NC(NCCCCCN4CCCC4)=C2C=C1OC.O=C(O)C(F)(F)F

4-Quinazolinamine, 6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-, 2,2,2-trifluoroacetate (1:x)

(-20℃)

With Ice Pack

≥ 2 years