MK-4101

SKU: orb1300372

Description

MK-4101

Research Area

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

Key Properties

• CAS Number: 935273-79-3
• MW: 493.47
• Purity: 96.07%
• Formula: C₂₄H₂₄F₅N₅O
• SMILES: Cn1c(nnc1C12CCC(CC1)(CC2)c1noc(n1)C1CC(F)(F)C1)-c1ccccc1C(F)(F)F
• Target: Smo,Hedgehog/Smoothened,Apoptosis
• 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