Bioactivity | PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer[1]. |
Target | IC50: 23 nM (PKM2) |
Invitro | PKM2-IN-6 (compound 7d) (0, 20, 40, 60, 80, 100 μM; 48 h) 对 COLO-205,A-549、MCF-7 细胞显示细胞毒性,IC50 值分别为 18.33、47.00、19.80 μM[1]。PKM2-IN-6 (14.38 μM; 48 h) 诱导细胞凋亡和细胞周期停滞在 G2 期[1]。PKM2-IN-6 (14.38 μM; 24 h) 可在 mRNA 水平上降低 PKM1 和 PKM2 的表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PKM2-IN-6 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
In Vivo | PKM2-IN-6 (25, 50 mg/kg; p.o.; daily for 3 weeks) 可减少小鼠的肿瘤体积和重量[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 771467-00-6 |
Formula | C17H14N4OS |
Molar Mass | 322.38 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Das R, et al. Mechanistic Investigation of Thiazole-Based Pyruvate Kinase M2 Inhibitor Causing Tumor Regression in Triple-Negative Breast Cancer. J Med Chem. 2024 Feb 26. |