TH287 |
| Catalog No.GC17601 |
TH287은 MTH1의 강력하고 선택적인 억제제이며 IC50은 0.8nM입니다. TH287은 100μM에서 MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase 및 ITPA의 관련 억제 없이 MTH1에 대해 고도로 선택적입니다. TH287은 암 연구를 위한 화학요법제로 작용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1609960-30-6
Sample solution is provided at 25 µL, 10mM.
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TH287 is a potent MTH1 inhibitor with IC50 of 0.8±0.1 nM. [1]
MTH1 (human MutT homolog 1) is an antimutagenic purine nucleoside triphosphatase that sanitize oxidized nucleotide pools. It’s a new cancer therapeutic target as it protects the cancer cell from DNA damages such as oxidative stress-induced cell dysfunction or death.
In U2OS and other cancer cell lines, TH287 treatment selectively and effectively kill cancer cells with less toxic to some primary or immortalized cells. U2OS cells treated with TH287 shows increase of 8-oxodG in DNA. The MTH1 inhibitor TH287 induces DNA damage and activates an ATM-p53-mediated death response and DNA repair in U2OS cells. [1]
Reference:
1. Gad H, Koolmeister T, Jemth AS et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21.
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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