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UNC0642

CAS No. : 1481677-78-4

MCE 站：UNC0642

产品活性：UNC0642是有效，选择性的赖氨酸甲基转移酶 G9a 和 GLP 抑制剂， 抑制 G9a 的IC₅₀ 值小于2.5 nM。

研究领域：Epigenetics

作用靶点：Histone Methyltransferase

In Vitro: UNC0642 displays high in vitro and cellular potency, low cell toxicity, and excellent selectivity. UNC0642 is competitive with the peptide substrate and non-competitive with the cofactor SAM. The K_i of UNC0642 is determined to be 3.7±1 nM. UNC0642 displays high in vitro potency for GLP (IC₅₀< 2.5 nM), similar to G9a. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. UNC0642 exhibits high potency at reducing the H3K9me2 mark, low cell toxicity, and good separation of functional potency and cell toxicity in a number of cell lines. It reduces clonogenicity in PANC-1 cells, a pancreatic carcinoma cell line.

In Vivo: A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642 results in a plasma C_max (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Reprogramming Compound Library  |  Chemical Probe Library  |  Anti-Blood Cancer Compound Library  |  3-Deazaneplanocin A hydrochloride  |  Chaetocin  |  UNC1999  |  MS023  |  BIX-01294  |  EPZ020411 hydrochloride  |  MM-102 TFA  |  SGC0946  |  A-366  |  Amodiaquine dihydrochloride dihydrate  |  CM-272  |  AZ505  |  SGC707  |  PFI-2 hydrochloride  |  NSC 663284  |  UNC0379  |  A-196  |  Sinefungin  |  SGC3027  |  AMI-1  |  EI1  |  BVT948  |  MS049  |  HLCL-61 hydrochloride  |  UNC0646  |  UNC 0631  |  UNC3866  |  BI-9321 trihydrochloride

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