XMD 8-92

Name: XMD 8-92
Brand: Tocris Bioscience
SKU: 4132

Tocris Bioscience, part of Bio-Techne | Catalog # 4132

Citations (11)

COA / SDS

ERK5/BMK1 inhibitor; also BRD4 inhibitor

Key Product Details

Description:	ERK5/BMK1 inhibitor; also BRD4 inhibitor
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
Purity:	≥98% (HPLC)
Molecular Weight:	474.55

View Full Technical Details for XMD 8-92

Technical Data
Citations

Biological Activity for XMD 8-92

XMD 8-92 is an ERK5 (BMK1) and BRD4 inhibitor (K_d values are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (K_d 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.

Compound Libraries for XMD 8-92

XMD 8-92 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

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.

Technical Data for XMD 8-92

M. Wt	474.55
Formula	C₂₆H₃₀N₆O₃
Storage	Store at RT
Purity	≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for XMD 8-92

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 will 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

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References for XMD 8-92

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