Network Version
TEPP-46 Data Sheet
| Product Name: | TEPP-46 |
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|---|---|---|
| CAS No.: | 1221186-53-3 | |
| Cat. No.: | HY-18657 | |
| MWt: | 372.46 | |
| Formula: | C17H16N4O2S2 | |
| Purity : | >98% | |
| Solubility: | DMSO : 50 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR[1][2][3]. In Vitro:TEPP-46 and DASA-58 activate PKM2 by a mechanism similar to that of the endogenous activator FBP. Pre-treatment of cells with TEPP-46 or DASA-58 prevents pervanadate-induced inhibition of PKM2 activity. TEPP-46 also induces a decrease in the intracellular levels of acetyl-coA, lactate, ribose phosphate and serine[1]. TEPP-46 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes. TEPP-46 treatment significantly downregulates the expression of the M1 markers Il12p40 and Cxcl-10. Activation of PKM2 using TEPP-46 significantly inhibits FSL-1 and CpG-induced Il1b mRNA expression. TEPP-46 inhibits Mtb-induced Il1b mRNA levels, boosts Mtb-induced levels of Il10 mRNA, and has no effect on levels of Tnf[2]. In Vivo:TEPP-46 exhibits good oral bioavailability with relatively low clearance, long half-life, and good volume of distribution-parameters that predict for drug exposure in tumor tissues. TEPP-46 at 150 mg/kg readily achieves maximal PKM2 activation measured in A549 xenograft tumors[1]. | ||
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