XMD8-92

SKU: orb1307342

Description

XMD8-92 is a potent and selective small-molecule inhibitor of BMK1/ERK5, exhibiting a high-affinity binding dissociation constant (Kd) of 80 nM. This compound is a valuable research tool for investigating the ERK5 signaling pathway in both cellular and animal models, particularly in studies related to cancer, cardiovascular biology, and inflammation.

Research Area

Cell Biology, Epigenetics & Chromatin, Metabolism Research, Molecular Biology, Neuroscience, Signal Transduction

Key Properties

• CAS Number: 1234480-50-2
• MW: 474.55
• Purity: 98.21% (May vary between batches)
• Formula: C₂₆H₃₀N₆O₃
• SMILES: CCOc1cc(ccc1Nc1ncc2N(C)C(=O)c3ccccc3N(C)c2n1)N1CCC(O)CC1
• Target: PPAR,CaMK,ERK,BMI-1,Epigenetic Reader Domain
• Solubility: DMSO:19 mg/mL (40.04 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.21 mM)

Bioactivity

• Target IC50:
  BRD4:190 nM (Kd)|BMK1:80 nM(Kd)
• In Vivo:
  Hydroxysafflor yellow A (HSYA) inhibits the activation of hepatic stellate cells, while XMD8-92 can significantly block this inhibition and prevent the HSYA-mediated downregulation of MEF2C. By inhibiting the activation of BMK1, XMD8-92 significantly induces the expression of p21 in cells and inhibits the proliferation of cancer cells.
• In Vitro:
  XMD8-92 significantly inhibits the growth of pancreatic tumor xenografts by downregulating DCLK1 and several of its downstream targets. At a dose of 50 mg/kg, administered intraperitoneally (i.p.), XMD8-92 blocks tumor cell proliferation and tumor-associated angiogenesis, resulting in significant suppression of tumor growth in both xenografted human and syngeneic mouse models.

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

cancer, bFGF, BMI-1, BMI1, inhibit, Extracellular signal regulated kinases, ERK, Epigenetic Reader Domain, EpigeneticReaderDomain, HMEC, leukemia, Inhibitor, protein, promyelocytic, XMD892, XMD-8-92, XMD8-92, XMD8 92

Compound Identifiers

PubChem CID

46843772