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SKU | Size | Availability | Price | Qty |
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M651697-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $150.90 | |
M651697-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $250.90 | |
M651697-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $650.90 | |
M651697-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $950.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 ( IC 50 =0.9 µM for CK1δ) and CHK1 ( IC 50 =0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 ( IC 50 =0.9 µM for CK1δ) and CHK1 ( IC 50 =0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation In Vitro MRT00033659 (5-40 µM; 48 hours) is sufficient to significantly reduce cell number of 5 µM. MRT00033659 (1-80 µM; 48 hours) induces substantial cell death from 5 µM. MRT00033659 (0.2-80 µM; 48 hours) induces a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 µM to 5 µM. MRT00033659 does not inhibit p38α MAPK. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A375 cells Concentration: 5, 20, 40 µM Incubation Time: 48 hours Result: Significantly reduced cell number of 5 µM. Apoptosis AnalysisCell Line: A375 cells Concentration: 1, 5, 10, 20, 40, 80 µM Incubation Time: 48 hours Result: Induced substantial cell death from 5 µM. Western Blot AnalysisCell Line: A375 cells Concentration: 0.2, 1, 5, 10, 20, 40, 80 µM Incubation Time: 48 hours Result: Induced a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 µM to 5 µM. Form:Solid IC50& Target:CKIδ 0.9 μM (IC 50 ) Chk1 0.23 μM (IC 50 ) |
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IUPAC Name | N-[3-(3-methyl-2H-pyrazolo[3,4-b]pyridin-5-yl)phenyl]acetamide |
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INCHI | InChI=1S/C15H14N4O/c1-9-14-7-12(8-16-15(14)19-18-9)11-4-3-5-13(6-11)17-10(2)20/h3-8H,1-2H3,(H,17,20)(H,16,18,19) |
InChi Key | YFBPGSDPFRCNOY-UHFFFAOYSA-N |
Canonical SMILES | CC1=C2C=C(C=NC2=NN1)C3=CC(=CC=C3)NC(=O)C |
Isomeric SMILES | CC1=C2C=C(C=NC2=NN1)C3=CC(=CC=C3)NC(=O)C |
PubChem CID | 66555775 |
Molecular Weight | 266.30 |
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Solubility | DMSO : 83.33 mg/mL (312.92 mM; Need ultrasonic) |
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