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SB 202190

Cat. No. M2062
SB 202190 Structure
Size Price Availability Quantity
50mg USD 120 In stock
100mg USD 150 In stock
200mg USD 200 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

SB 202190 is a potent p38 MAPK inhibitor. SB 202190 binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38α and β isoforms (IC50 = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38β2 respectively). SB 202190 by itself was sufficient to induce cell death, with typical apoptotic features such as nucleus condensation and intranucleosomal DNA fragmentation. SB 202190 stimulated the activity of CPP32-like caspases, and its apoptotic effect was completely blocked by the expression of bcl-2. When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs). Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 331.34
Formula C20H14FN3O
CAS Number 152121-30-7
Purity >98%
Solubility DMSO 50 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Br J Pharmacol (2006). Figure 1. SB 202190
Method FLIPR
Cell Lines HEK293 cells
Concentrations 10 μM
Incubation Time 18 h
Results The MAPK inhibitor, SB-202190, also antagonized human P2X7 receptor-mediated responses but was generally less potent than SB-203580 with pIC50 values varying from 6.2 to 4.8, depending on BzATP concentration.
Rating
References

Targeting the p38 MAPK pathway inhibits irinotecan resistance in colon adenocarcinoma.
Paillas S, et al. Cancer Res. 2011 Feb 1;71(3):1041-9. PMID: 21159664.

Activation of c-Jun N-terminal kinase (JNK) by widely used specific p38 MAPK inhibitors SB202190 and SB203580: a MLK-3-MKK7-dependent mechanism.
Muniyappa H, et al. Cell Signal. 2008 Apr;20(4):675-83. PMID: 18222647.

Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase.
Nemoto S, et al. J Biol Chem. 1998 Jun 26;273(26):16415-20. PMID: 9632706.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB 202190 supplier, p38 MAPK, inhibitors

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