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565852 PTP Inhibitor XXXI, II-B08 - Calbiochem

PTP Inhibitor XXXI, II-B08, is a cell-permeable compound that targets SHP2 catalytic domain and inhibit SHP2-catalyzed pNPP hydrolysis (IC50 = 5.5 µM) in a reversible, non-competitive manner.

PTP Inhibitor XXXI, II-B08 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: CD45 Inhibitor V, FAP1 Inhibitor, LMWPTP Inhibitor, Lyp Inhibitor III, PTP1B Inhibitor IX, SHP1 Inhibitor IX, 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, SHP2 Inhibitor VI

Primary Target: SHP2
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Přehled

Replacement Information

Tabulka spec. kláve

Empirical Formula
C₃₃H₂₇N₅O₄
Description
OverviewA 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.
Catalogue Number565852
Brand Family Calbiochem®
SynonymsCD45 Inhibitor V, FAP1 Inhibitor, LMWPTP Inhibitor, Lyp Inhibitor III, PTP1B Inhibitor IX, SHP1 Inhibitor IX, 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, SHP2 Inhibitor VI
References
ReferencesMali, R.S., et al. 2012. Blood 120, 2669.
Zhang, X., et al. 2010. J. Med. Chem. 53, 2482.
Product Information
FormYellowish white powder
Hill FormulaC₃₃H₂₇N₅O₄
Chemical formulaC₃₃H₂₇N₅O₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ200
Applications
ApplicationPTP Inhibitor XXXI, II-B08, is a cell-permeable compound that targets SHP2 catalytic domain and inhibit SHP2-catalyzed pNPP hydrolysis (IC50 = 5.5 µM) in a reversible, non-competitive manner.
Biological Information
Primary TargetSHP2
Primary Target IC<sub>50</sub>5.5, 9.0 and 10.8 µ
Primary Target K<sub>i</sub>5.2 µ
Secondary targetOther PTPs
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalogové číslo GTIN
565852 0

Documentation

PTP Inhibitor XXXI, II-B08 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

PTP Inhibitor XXXI, II-B08 - Calbiochem Certificates of Analysis

TitleLot Number
565852

References

Přehled odkazů
Mali, R.S., et al. 2012. Blood 120, 2669.
Zhang, X., et al. 2010. J. Med. Chem. 53, 2482.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision16-April-2013 JSW
SynonymsCD45 Inhibitor V, FAP1 Inhibitor, LMWPTP Inhibitor, Lyp Inhibitor III, PTP1B Inhibitor IX, SHP1 Inhibitor IX, 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, SHP2 Inhibitor VI
DescriptionA 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.
FormYellowish white powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₃H₂₇N₅O₄
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesMali, R.S., et al. 2012. Blood 120, 2669.
Zhang, X., et al. 2010. J. Med. Chem. 53, 2482.