Home Stem Cells & Wnt Hedgehog/Smoothened inhibitor MK-4101 For research use only.

MK-4101

MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.

MK-4101 Chemical Structure

MK-4101 Chemical Structure

CAS No. 935273-79-3

Purity & Quality Control

Batch: S820001 DMSO]98 mg/mL]false]Ethanol]98 mg/mL]false]Water]Insoluble]false Purity: 99.33%
99.33

MK-4101 Related Products

Signaling Pathway

Hedgehog/Smoothened Signaling Pathways

Hedgehog/Smoothened Signaling Pathway

Biological Activity

Description MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.
Targets
SMO [1]
In vitro
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].
Cell Research Cell lines BCC(basal cell carcinoma) cells
Concentrations 10 μM
Incubation Time 72 h
Method BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation.
In Vivo
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].
Animal Research Animal Models C57bl/6 mice or Sprague-Dawley rats.
Dosages 40 or 80 mg/kg once a day; 80 mg/kg twice a day
Administration oral administration

Chemical Information & Solubility

Molecular Weight 493.47 Formula

C24H24F5N5O
CAS No. 935273-79-3 SDF Download MK-4101 SDF
Smiles CN1C(=NN=C1C23CCC(CC2)(CC3)C4=NOC(=N4)C5CC(C5)(F)F)C6=CC=CC=C6C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 98 mg/mL ( (198.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 98 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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