|Solubility:||DMSO up to 100 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
SCH51344 is a novel potent, selective and cell permeable inhibitor of the nudix hydrolase family MTH1 protein with an IC50 of ~49 nM. It inhibits Ras-induced malignant transformation. It has no effect on Ras-induced ERK and JNK activation. SCH51344 inhibits Ras-induced membrane ruffling in REF-52 fibroblasts and blocks anchorage-independent growth of Ras-transformed tumor cell lines. It also induces DNA damage in SW480 colon cancer cells. Loss-of-function of MTH1 impaired growth of KRAS tumor cells, whereas MTH1 overexpression mitigated sensitivity towards SCH51344.
How to Use:
- In vitro: SCH51344 was used at 5-20 µM final concentration in various in vitro and cellular assays.
- In vivo: n/a
- 1. Kumar CC, et al. SCH 51344 inhibits ras transformation by a novel mechanism. (1995) Cancer Res. 55, 5106–5117.
- 2. Walsh AB, et al. SCH 51344-induced reversal of RAS-transformation is accompanied by the specific inhibition of the RAS and RAC-dependent cell morphology pathway. (1997) Oncogene. 15(21):2553-60.
- 3. Kumar CC, et al. SCH 51344, an inhibitor of RAS/RAC-mediated cell morphology pathway. (1999) Ann N Y Acad Sci. 886:122-31.
- 4. Huber KV, et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. (2014) Nature. 508(7495):222-7.
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