HDAC-IN-46 (compound 12c) 是一种有效的HDAC抑制剂,对 HDAC1 和 HDAC6 的IC50分别为 0.21 μM 和 0.021 μM。HDAC-IN-46 在 MDA-MB-231 细胞中上调 p-p38,下调 BCL-xL 和 cyclin D1。HDAC-IN-46诱导细胞周期 G2 期阻滞和细胞凋亡 (Apoptosis)。HDAC-IN-46 可用于研究三阴性乳腺癌 (TNBC)。
产品描述
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC 50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) [1].
体外活性
HDAC-IN-46 (compound 12c) has antiproliferative activity against MDA-MB-231, A549 and MCF-7 with IC 50 s of 88.46±10.5 μM, 83.34 ± 15.5 μM and 21.4±3.7 μM, respectively [1]. HDAC-IN-46 (5, 12.5 and 25 μM; 24 h) causes concentration-dependent upregulation of p-p38 and downregulation of Bcl-xL and cyclin D1 in MDA-MB-231 cells [1]. HDAC-IN-46 (12.5 and 25 μM; 48 h) induces significant G2 phase arrest and apoptosis [1]. Western Blot Analysis [1] Cell Line: MDA-MB-231 cells Concentration: 5, 12.5 and 25 μM Incubation Time: 24 h Result: Caused concentration-dependent upregulation of p-p38 and downregulation of Bcl-xL and cyclin D1. Cell Cycle Analysis [1] Cell Line: MDA-MB-231 cells Concentration: 12.5 and 25 μM Incubation Time: 48 h Result: Induced significant G2 phase arrest and apoptosis.
Cas No.
2562386-85-8
分子式
C22H30N8O2
分子量
438.53
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years