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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, CAS 1234480-50-2

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Purity: 98%

Biological Description

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Description	XMD8-92 is an effective and specific BMK1/ERK5 inhibitor (Kd: 80 nM).
Targets&IC50	BMK1:80 nM(Kd)
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	474.565
Formula	C26H30N6O3
CAS No.	1234480-50-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 19 mg/mL (40 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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-Cancer Compound Library Autophagy Compound Library Anti-Cancer Metabolism Compound Library Anti-Obesity Compound Library Glutamine Metabolism Compound Library Inhibitor Library DNA Damage & Repair Compound Library Cell Cycle Compound Library Kinase Inhibitor Library Stem Cell Differentiation Compound Library

Related Products

Related compounds with same targets

PTC-209 hydrobromide PRT4165 PTC-209 XMD8-92 PTC-028 Unesbulin

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

XMD8-92 1234480-50-2 DNA损伤和修复 MAPK信号通路表观遗传细胞周期 BMI-1 Epigenetic Reader Domain ERK Extracellular signal regulated kinases XMD-8-92 bFGF Inhibitor promyelocytic XMD8 92 protein cancer XMD892 inhibit leukemia HMEC inhibitor

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