526527
PIM Kinase Inhibitor VIII, R8-T198wt
The PIM Kinase Inhibitor VIII, R8-T198wt controls the biological activity of PIM Kinase. This small molecule/inhibitor is primarily used for Cancer applications.
Synonym(s):
PIM Kinase Inhibitor VIII, R8-T198wt, NH2-GGGRRRRRRRRGC~KKPGLRRRQT-CO2H, cpm-P27kip1189-198
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About This Item
Empirical Formula (Hill Notation):
C111H211N59O26S
Molecular Weight:
2820.31
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Quality Segment
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
white
solubility
DMSO: 50 mg/mL, clear, colorless (Use only fresh DMSO.), water: 50 mg/mL, clear, colorless
shipped in
ambient
storage temp.
−20°C
General description
The human p27Kip1 C-terminus PIM-1 phosphorylation site- (Thr198) containing sequence is synthesized with an N-terminal Arg octamer/R8-containing sequence to facilitate its use as a cell-permeable, substrate-competitive PIM-1 inhibitor. Reported to retard human prostate carcinoma DU145-derived tumor growth in mice (100% vs 257% tumor growth on day 14 with or without 0.5 µmol/animal dosing on days 0 & 3; intratumoral injection) in vivo and completely prevents tumor expansion for up to 17 days (0.5 µmol/animal on days 0 & 5; intratumoral injection) when combined with a single Taxol (Cat. No. 580555) dosage (60 mg/kg; i.p.) on day zero. Studies using FITC-conjugated R8-T198wt confirms cellular delivery and PIM-1 interaction (KD = 323 nM), demonstrating also that R8-T198wt-induced cell cycle arrest and apoptosis in PIM-1-expressing DU145 cells are direct consequences of inhibition of PIM-1-mediated p27Kip1 Thr198 and Bad Ser112 phosphorylation, respectively.
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
H-Gly-Gly-Gly-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Cys-Lys-Lys-Pro-Gly-Leu-Arg-Arg-Arg-Gln-Thr-OH
Morishita, D., et al. 2011. J. Biol. Chem.286, 2681.
Morishita, D., et al. 2008. Cancer Res.68, 5076.
Morishita, D., et al. 2008. Cancer Res.68, 5076.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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