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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  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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  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 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

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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.

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

Conversion of different model animals based on BSA (PMID: 27057123)

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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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.