SB 202190

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.

Product Citations

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  Patent. CN116286654A 2024-01-30.

  Patent. CN116286654A
  SB 202190 purchased from AbMole

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  Patent. CN116286654A 2024 Jan 30; .

  Patent. CN116286654A
  SB 202190 purchased from AbMole

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  Immunol Invest. 2023 Apr;52(3):298-318.

  All-Trans Retinoic Acid Promotes M2 Macrophage Polarization in Vitro by Activating the p38MAPK/STAT6 Signaling Pathway
  SB 202190 purchased from AbMole

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  Patent. CN117074141A 2023 Nov 17.

  Patent. CN117074141A
  SB 202190 purchased from AbMole

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  Patent. CN114606192B 2023 Aug 08.

  Patent. CN114606192B
  SB 202190 purchased from AbMole

• 

  Patent. CN114606192A 2023-08-08.

  Patent. CN114606192A
  SB 202190 purchased from AbMole

• 

  Patent. CN114606192A 2023 Aug 08; .

  Patent. CN114606192A
  SB 202190 purchased from AbMole

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  Cell Death Dis. 2022 Apr 5;13(4):303.

  KLF5 inhibition overcomes oxaliplatin resistance in patient-derived colorectal cancer organoids by restoring apoptotic response
  SB 202190 purchased from AbMole

• 

  Research Square. 2022 Feb.

  Dexmedetomidine preconditioning alleviates H2O2-induced oxidative stress and apoptosis in human umbilical vein endothelial cells via p38MAPK signaling pathway
  SB 202190 purchased from AbMole

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  Cell Stem Cell. 2020 Nov 5;27(5):840-851.e6.

  Next-Generation Surrogate Wnts Support Organoid Growth and Deconvolute Frizzled Pleiotropy In Vivo
  SB 202190 purchased from AbMole

• 

  Oncology. 2020 Jul 20.

  5-Fluorouracil enhances the chemosensitivity of gastric cancer to TRAIL via inhibition of the MAPK pathway
  SB 202190 purchased from AbMole

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.

Protocol (for reference only)

Cell Experiment
Cell lines	R28 cells
Preparation method	R28 cells were seeded into 12-well culture plates (1 × 10^5 cells/well) and divided into four groups: the control group, glutamate group (10 mM glutamate), SB202190 group (10 mM glutamate + 25 µM SB202190) and ferrostatin-1 group (glutamate 10 mM + 1 µM ferrostatin-1).
Concentrations	25 µM
Incubation time	24 hours

Animal Experiment
Animal models	NOD/LtJ mice
Formulation	Not mentioned
Dosages	5 mg/kg
Administration	Intraperitoneal injection

Chemical Information

Molecular Weight	331.34
Formula	C20H14FN3O
CAS Number	152121-30-7
Solubility (25°C)	DMSO 36 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Paillas S, et al. Cancer Res. Targeting the p38 MAPK pathway inhibits irinotecan resistance in colon adenocarcinoma.

[2] Muniyappa H, et al. Cell Signal. Activation of c-Jun N-terminal kinase (JNK) by widely used specific p38 MAPK inhibitors SB202190 and SB203580: a MLK-3-MKK7-dependent mechanism.

[3] Nemoto S, et al. J Biol Chem. Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase.