526526
PIM3 Kinase Inhibitor VII, M-110
Synonym(s):
PIM3 Kinase Inhibitor VII, M-110, Nʹ-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide
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About This Item
Empirical Formula (Hill Notation):
C22H28ClN5O3
Molecular Weight:
445.94
NACRES:
NA.28
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 50 mg/mL
shipped in
wet ice
storage temp.
−20°C
General description
A cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (Ki = 0.3 µM), and highly isoform-selective PIM inhibitor (IC50 = 2.5, 2.5, and 0.047 µM against PIM1, PIM2, and PIM3, respectively, with PIMtide as substrate, [ATP] = 10 µM), while affecting CK2α2 only at much higher concentrations (IC50 = 5 µM, [ATP] = 10 µM) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition; [M-110] = 5 µM). M-100 treatment (10 µM for 18 hr) is shown to inhibit both basal (by 73% and 83% of DMSO control in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells, respectively) and IL-6-stimulated (by 69% of DMSO control in DU-145 cells) STAT3 phosphorylation on Tyr705, while displaying little effect toward Tyr694 phosphoylation (in 22RV1 cultures). Isoform-specific knockdowns in DU-145 cells likewise identify PIM-3, but not PIM-1 or -2, as the kinase responsible for cellular STAT3 Tyr705 phosphorylation.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Chang, M., et al. 2010. Mol. Cancer Ther.9, 2478.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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