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565852

Sigma-Aldrich

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.

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C33H27N5O4
Molecular Weight:
557.60
UNSPSC Code:
12352200

Quality Level

200

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

storage temp.

2-8°C

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.
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). Effectively blocks SHP2-mediated human hematopoietic progenitor cell hyperproliferation (10 µM) due to SHP2 mutations (D61Y and E76K) or GM-CSF stimulation, as well as c-kit-dependent (due to D814V mutation or via ligand stimulation), SHP2-mediated myeloid proliferation (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 of mice bearing D814V KIT-expressing 32D cells in vivo.

Biochem/physiol Actions

Primary Target
SHP2
Reversible: yes
Secondary Target
Other PTPs
Target IC50: 5.5, 9.0 and 10.8 &micro

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Legal Information

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

wgk_germany

WGK 2

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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