| Bioactivity | UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications[1][3]. | ||||||||||||
| Invitro | UNC0321 (Compound 29) 抑制 G9a ECSD、G9a CLOT、GLP ECSD 和 GLP CLOT 的活性，IC50 值分别为 9 nM、6 nM、15 nM 和 23 nM。UNC0321 (Compound 3) 降低了 MDA-MB-231 细胞中 H3K9me2 的水平，IC50 值为 11 µM[2]。UNC0321 (200 pM；48 h) 显著抑制 Rab4 在 HUVEC 中的表达[3]。 Western Blot Analysis[3] Cell Line: | ||||||||||||
| Name | UNC0321 | ||||||||||||
| CAS | 1238673-32-9 | ||||||||||||
| Formula | C27H45N7O3 | ||||||||||||
| Molar Mass | 515.69 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57. [2]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50. [3]. Nie J. UNC0321 inhibits high glucose induced apoptosis in HUVEC by targeting Rab4. Biomed Pharmacother. 2020 Nov;131:110662. |