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XMD8-92

Catalog No. T1843   CAS 1234480-50-2

XMD8-92 is an effective and specific BMK1/ERK5 inhibitor (Kd: 80 nM).

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XMD8-92 Chemical Structure
XMD8-92, CAS 1234480-50-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 48.00
10 mg In stock $ 68.00
25 mg In stock $ 133.00
50 mg In stock $ 247.00
100 mg In stock $ 413.00
1 mL * 10 mM (in DMSO) In stock $ 51.00
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Purity: 98.19%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description XMD8-92 is an effective and specific BMK1/ERK5 inhibitor (Kd: 80 nM).
Targets&IC50 BMK1:80 nM(Kd)
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.
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.
Kinase Assay KiNativ profiling of XMD8-92 is carried out with both an ATP and ADP acylphosphate-desthiobiotin with the following modifications. HeLa cell lysates (5 mg/mL total protein) are incubated in the presence of XMD8-92 at 50 μM, 10 μM, 2 μM, 0.8 μM, and 0 μM for 15 minutes prior to addition of the ATP or ADP acylphosphate probe (5 μM final probe concentration). All reactions are performed in duplicate. Probe reactions proceeded for 10 minutes and the reaction stopped by the addition of urea and processed for MS analysis. Samples are analyzed by LC-MS/MS on a linear ion trap mass spectrometer using a time segmented "target list" designed to collect MS/MS spectra from all kinase peptide-probe conjugates that can be detected in HeLa cell lysates. This target list is generated and validated by prior exhaustive analysis of HeLa lysates. Up to four characteristic fragment ions for each kinase peptide-probe conjugate are used to extract signals for each kinase, and a comparison of inhibitor treated to control (untreated) lysates allow for precise determination of % inhibition at each point. A manuscript describing the details of this targeted mass spectrometry approach is in preparation[1].
Molecular Weight 474.55
Formula C26H30N6O3
CAS No. 1234480-50-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 19 mg/mL (40 mM)

TargetMolReferences and Literature

1. Yang Q, et al. Cancer Cell. 2010, 18(3), 258-267. 2. Dong H, et al. Pharm Biol. 2013. doi:10.3109/13880209. 3. Sureban SM, et al. Cancer Lett. 2014 , 351(1), 151-161.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Pancreatic Cancer Compound Library Autophagy Compound Library Target-Focused Phenotypic Screening Library Reprogramming Compound Library Bioactive Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Inhibitor Library Highly Selective Inhibitor Library Anti-Obesity Compound Library

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Keywords

XMD8-92 1234480-50-2 Cell Cycle/Checkpoint Chromatin/Epigenetic DNA Damage/DNA Repair MAPK Epigenetic Reader Domain BMI-1 ERK Extracellular signal regulated kinases XMD-8-92 bFGF Inhibitor promyelocytic XMD8 92 protein cancer XMD892 inhibit leukemia HMEC inhibitor

 

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