565852
PTP Inhibitor XXXI, II-B08
The PTP Inhibitor XXXI, II-B08 controls the biological activity of PTP. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
PTP Inhibitor XXXI, II-B08, CD45 Inhibitor V, FAP1 Inhibitor, LMWPTP Inhibitor, Lyp Inhibitor III, PTP1B Inhibitor IX, SHP1 Inhibitor IX, SHP2 Inhibitor VI, 3-(1-(3-(Biphenyl-4-ylamino)-3-oxopropyl)-1H-1,2,3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1H-indole-5-carboxylic acid
assay
≥98% (HPLC)
form
powder
potency
5.2 μM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow-white
solubility
DMSO: 100 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable indolo-salicylic acid compound that is shown to target SHP2 catalytic domain and inhibit SHP2-catalyzed pNPP hydrolysis (IC50 = 5.5 µM) in a reversible and non-competitive manner (Ki = 5.2 µM), exhibiting 2.6- to 5.7-fold selectivity over PTP1B, SHP1, FAP1, Lyp, CD45, and LMWPTP (IC50 = 14.3, 15.7, 20.3, 25.0, 30.0, and 31.1 µM, respectively) and >9-fold selectivity over Cdc14A, HePTP, LAR, PTPα, and VHR (IC50 >50 µM). Effectively blocks hyperproliferative activity of human hematopoietic progenitor cells (Effective conc. = 10 µM) due to SHP2 mutations (D61Y and E76K) or GM-CSF stimulation, as well as c-kit-dependent (via ligand stimulation or D814V mutation), SHP2-mediated myeloid proliferation (Effective conc. = 5 to 75 µM). Dual PI-3K and SHP2 inhibition by LY294002 (Cat. Nos. 440202 & 440204) and II-B08 (10 mg/kg and 50 mg/kg, respectively; daily i.p.) is shown to greatly prolong the survival rate in a D814V KIT-expressing 32D-based murine MPD (myeloproliferative disease) model (0% survival rate on day 23, 27, 28, respectively, with DMSO, LY294002, II-B08 treatment alone; 20% survival rate on day 65 with combined treatment) in vivo.
Biochem/physiol Actions
Primary Target
SHP2
SHP2
Reversible: yes
Secondary Target
Other PTPs
Other PTPs
Target IC50: 5.5, 9.0 and 10.8 µ
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
Mali, R.S., et al. 2012. Blood120, 2669.
Zhang, X., et al. 2010. J. Med. Chem.53, 2482.
Zhang, X., et al. 2010. J. Med. Chem.53, 2482.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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