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526527

Sigma-Aldrich

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-P27 Kip1189-198, 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

Quality Level

100

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

Warning

Toxicity: Regulatory Review (Z)

Sequence

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

Physical form

Supplied as a trifluoroacetate salt

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Morishita, D., et al. 2011. J. Biol. Chem.286, 2681.
Morishita, D., et al. 2008. Cancer Res.68, 5076.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

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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