XMD 8-92
Tocris Bioscience, part of Bio-Techne | Catalog # 4132
ERK5/BMK1 inhibitor; also BRD4 inhibitor
Product Description
XMD 8-92 is an ERK5 (BMK1) and BRD4 inhibitor (Kd values are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (Kd values are 190, 600 and 890 nM). Blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity in in vitro kinase assays. Also reduces BMK1-dependent transactivating activity of MEF2C. Inhibits proliferation in a variety of cancer cell lines; blocks tumor cell proliferation and tumor-associated angiogenesis.Licensing Information
Sold under license from the Dana-Farber Cancer Institute.External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of XMD 8-92 is reviewed on the chemical probes website.Product Specifications
Molecular Weight
474.55
Formula
C26H30N6O3
Storage
Store at RT
Purity
≥98% (HPLC)
Chemical Name
2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
CAS Number
1234480-50-2
PubChem ID
46843772
InChI Key
QAPAJIZPZGWAND-UHFFFAOYSA-N
SMILES
O=C2C3=C(C=CC=C3)N(C)C1=NC(NC4=C(OCC)C=C(N5CCC(O)CC5)C=C4)=NC=C1N2C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.98 | 40 |
Preparing Stock Solutions
for XMD 8-92
The following data is based on the product molecular weight 474.55
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.4 mM | 5.27 mL | 26.34 mL | 52.68 mL |
| 2 mM | 1.05 mL | 5.27 mL | 10.54 mL |
| 4 mM | 0.53 mL | 2.63 mL | 5.27 mL |
| 20 mM | 0.11 mL | 0.53 mL | 1.05 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Lin ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc.Natl.Acad.Sci.U.S.A. 2016 PMID: 27679845
- Erazo Canonical and kinase activity-independent mechanisms for extracellular signal-regulated kinase 5 (ERK5) nuclear translocation require dissociation of Hsp90 from the ERK5-Cdc37 complex. Mol.Cell Biol. 2013 PMID: 23428871
- Yang and Lee Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin.Cancer Res. 2011 PMID: 21385929
- Deng Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a potent and selective inhibitor of big MAP kinase 1. ACS Med.Chem.Lett. 2011 PMID: 21412406
- Yang Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell 2010 PMID: 20832753
Product Specific Notices for XMD 8-92
For research use only
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