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MK-4101

Catalog No. T6891   CAS 935273-79-3

MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells.

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MK-4101 Chemical Structure
MK-4101, CAS 935273-79-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 39.00
5 mg In stock $ 68.00
10 mg In stock $ 113.00
25 mg In stock $ 213.00
50 mg In stock $ 343.00
100 mg In stock $ 571.00
500 mg In stock $ 1,230.00
1 mL * 10 mM (in DMSO) In stock $ 74.00
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Purity: 98.91%
Purity: 96.07%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells.
Targets&IC50 293 cells:1.1 µM (IC50), KYSE180 oesophageal cancer cells:1 µM (IC50), mouse cells:1.5 µM (IC50)
In vitro MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line (Gli_Luc) with IC50 = 1.5 μM and in human KYSE180 oesophageal cancer cells with an IC50 = 1 μM. Furthermore, MK-4101 displaced a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 = 1.1 μM. MK-4101 arrests cells in G1 and G2 phases[1].
In vivo MK-4101 has robust antitumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. MK-4101 is highly efficacious against primary medulloblastoma and basal cell carcinoma(BCC) developing in the cerebellum and skin of Ptch1+/- mice. Pharmacokinetics of MK-4101 shows that it could be administered orally, showing a good bioavailability (F ≥ 87 %) with low-to-moderate plasma clearance in mice and rats. Moreover, it was well absorbed, and mainly excreted into the bile[1].
Kinase Assay Luciferase assays: After various compound treatments, cells are lysed in luciferase lysis buffer and assayed for luciferase activity using the ONE-Glo luciferase assay system. All luciferase activities are normalized to protein concentration determined by Bradford assay.
Cell Research BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation. (Only for Reference)
Molecular Weight 493.47
Formula C24H24F5N5O
CAS No. 935273-79-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 60 mg/mL (121.6 mM)

DMSO: 92 mg/mL (186.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Filocamo G, et al. Mol Cancer Ther. 2016, 15(6):1177-89.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Prostate Cancer Compound Library Bioactive Compound Library Clinical Compound Library Osteogenesis Compound Library Apoptosis Compound Library Anti-Aging Compound Library

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Keywords

MK-4101 935273-79-3 Apoptosis GPCR/G Protein Stem Cells Hedgehog/Smoothened Smo MK4101 inhibit Smoothened Hedgehog MK 4101 Inhibitor inhibitor

 

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