MK-4101

SKU: orb1300372

Description

MK-4101 is a potent small molecule Hedgehog pathway inhibitor that suppresses tumor cell proliferation and induces apoptosis. It is utilized in cancer research for both in vitro mechanistic studies and in vivo models of Hedgehog-driven malignancies.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 935273-79-3
• MW: 493.47
• Purity: 99.13% (May vary between batches)
• Formula: C₂₄H₂₄F₅N₅O
• SMILES: Cn1c(nnc1C12CCC(CC1)(CC2)c1noc(n1)C1CC(F)(F)C1)-c1ccccc1C(F)(F)F
• Target: Apoptosis,Smo,Hedgehog/Smoothened
• Solubility: Ethanol:60 mg/mL (121.59 mM);DMSO:92 mg/mL (186.43 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.69 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HEK293 cells:1.1 µM (IC50)|KYSE180 oesophageal cancer cells:1 µM (IC50)|Mouse cells:1.5 µM (IC50)
• 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.
• In Vitro:
  MK-4101 inhibits Hh signaling with an IC50 of 1.5 μM in a reporter gene assay (Gli_Luc) in an engineered mouse cell line and 1 μM in human KYSE180 esophageal cancer cells. It displaces a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 μM. MK-4101 arrests cells in G1 and G2 phases.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, Inhibitor, Hedgehog, MK4101, MK-4101, MK 4101, inhibit, Smoothened, Smo

Compound Identifiers

PubChem CID

16222379