1. Stem Cell/Wnt
    Apoptosis
  2. Smo
    Apoptosis
    Hedgehog
  3. MK-4101

MK-4101 

Cat. No.: HY-100036 Purity: 98.13%
Handling Instructions

MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.

For research use only. We do not sell to patients.

MK-4101 Chemical Structure

MK-4101 Chemical Structure

CAS No. : 935273-79-3

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10 mM * 1 mL in DMSO USD 109 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis[1].

IC50 & Target

IC50: 1.1 µM (293 cells ); 1.5 µM (mouse cells); 1 µM (KYSE180 oesophageal cancer cells)[1]

In Vitro

MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line with an IC50 of 1.5 µM, and in human KYSE180 oesophageal cancer cells with an IC50 of 1 µM. MK-4101 displaces a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 µM, implying that the compound binds to SMO. MK4101 also inhibits the proliferation of medulloblastoma cells derived from neonatallyirradiated Ptch1-/+ mice in vitro with an IC50 of 0.3 µM[1].
MK-4101 (10 µM; 60 hours, 72 hours; medulloblastoma or BCC cells) treatment shows cell cycle arrest with a nearly complete disappearance of the S phase subpopulation, a prominent increase of the G1 population and, to a minor extent, of the G2 population[1].
MK-4101 (10 µM; medulloblastoma or BCC cells) treatment significantly reduces cyclin D1 protein and accumulation of cyclin B1 protein[1].

Cell Cycle Analysis[1]

Cell Line: Medulloblastoma or BCC cells
Concentration: 10 µM
Incubation Time: 60 hours, 72 hours
Result: Showed cell cycle arrest.

Western Blot Analysis[1]

Cell Line: Medulloblastoma or BCC cells
Concentration: 10 µM
Incubation Time:
Result: Significant reduction of cyclin D1 protein and accumulation of cyclin B1 protein.
In Vivo

MK-4101 (40-80 mg/kg; oral administration; for 3.5 weeks; CD1 nude female mice) treatment shows tumor growth inhibition (40 and 80 mg/kg ) and tumor regression at the highest dose (80 mg/kg). MK-4101 treatment shows a dose-dependent down-regulation of Gli1 mRNA. The maximum effect for tumor inhibition and hedgehog pathway downregulation is achieved at 80 mg/kg[1].

Animal Model: 5-weeks old CD1 nude female mice with medulloblastoma/BCC cells[1]
Dosage: 40 or 80 mg/kg once a day, 80 mg/kg twice a day
Administration: Oral administration; for 3.5 weeks
Result: Showed tumor growth inhibition (40 and 80 mg/kg ) and tumor regression at the highest dose (80 mg/kg).
Molecular Weight

493.47

Formula

C₂₄H₂₄F₅N₅O

CAS No.

935273-79-3

SMILES

FC(C1=CC=CC=C1C2=NN=C(C34CCC(C5=NOC(C6CC(F)(F)C6)=N5)(CC4)CC3)N2C)(F)F

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (101.32 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0265 mL 10.1323 mL 20.2647 mL
5 mM 0.4053 mL 2.0265 mL 4.0529 mL
10 mM 0.2026 mL 1.0132 mL 2.0265 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.13%

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