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MK-4101

MK-4101
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Purity:98.91%
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MK-4101

Catalog No. T6891Cas No. 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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Pack SizePriceAvailabilityQuantity
2 mg$39In Stock
5 mg$68In Stock
10 mg$113In Stock
25 mg$213In Stock
50 mg$343In Stock
100 mg$571In Stock
500 mg$1,230In Stock
1 mL x 10 mM (in DMSO)$74In Stock
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Product Introduction

Bioactivity
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.
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)
Chemical Properties
Molecular Weight493.47
FormulaC24H24F5N5O
Cas No.935273-79-3
Storage & Solubility Information
StoragePowder: -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)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.0265 mL10.1323 mL20.2647 mL101.3233 mL
5 mM0.4053 mL2.0265 mL4.0529 mL20.2647 mL
10 mM0.2026 mL1.0132 mL2.0265 mL10.1323 mL
20 mM0.1013 mL0.5066 mL1.0132 mL5.0662 mL
50 mM0.0405 mL0.2026 mL0.4053 mL2.0265 mL
100 mM0.0203 mL0.1013 mL0.2026 mL1.0132 mL

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