SCH51344, MTH1 Inhibitor


Catalog No. size PriceQuantity
M60212-2S 2 mg solid $139
M60212-10S 10mg solid $563

Description

Product Information
Molecular Weight: 316.36
Formula: C16H20N4O3
Purity: ≥98%
CAS#: 171927-40-5
Solubility: DMSO up to 100 mM
Chemical Name: 2-(2-((6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-yl)amino)ethoxy)ethanol
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:
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 

 

 

Reference: 

  • 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.

 


 


Products are for research use only. Not for human use. 

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