SB-202190

SKU: orb1305747

Description

SB 202190 is a potent, cell-permeable, and selective inhibitor of p38α and p38β2 MAP kinases. This compound is widely used in research to study inflammation, apoptosis, and cellular stress responses, and it has demonstrated utility in both in vitro models, such as stem cell differentiation into cardiomyocytes, and in vivo antitumor studies.

Research Area

Cell Biology, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 152121-30-7
• MW: 331.35
• Purity: >98%
• Formula: C₂₀H₁₄N₃OF
• SMILES: Oc1ccc(cc1)-c1nc(c([nH]1)-c1ccc(F)cc1)-c1ccncc1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 30 mg/ml).

Bioactivity

• Target IC50:
  p38α:50 nM (cell free)|U-CH1 cells:27.73 ± 13.16 μM|Astrocytes:64.8 μM|p38β:100 nM (cell free)
• In Vivo:
  METHODS: To investigate the role of p38 MAPK in mice with acute endotoxemia, SB 202190 (2 mg/kg) was injected intraperitoneally into C57BL/6 mice, followed by LPS (10 mg/kg) 30 min later. RESULTS: Pretreatment with SB 202190 significantly reversed LPS-induced left ventricular depression and reduced LPS-induced mortality by decreasing TNF-α levels. METHODS: In order to detect anti-tumor activity in vivo, SB 202190 (5 mg/kg) and OSI-027 (10 mg/kg) were injected intraperitoneally into BALB/c mice bearing human CRC tumor SW620 once a day for ten days. RESULTS: SB 202190 alone enhanced tumor proliferation and tumor load of SW620 xenografts. the combination of SB 202190 and OSI-027 significantly attenuated xenograft tumor growth.
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• In Vitro:
  METHODS: Human Tenon fibroblasts were treated with SB 202190 (5-50 μM) and cell viability was measured by MTT assay. RESULTS: SB 202190 is toxic to cells with an IC50 of 17.2 μM. METHODS: Human umbilical vein endothelial cells HUVEC were treated with SB 202190 (0.1-10 μM) for 6-48 h, and the expression levels of target proteins were detected by Western Blot method. RESULTS: After incubation with SB 202190 for 24 h, conversion of LC3A/B-I to PE-coupled LC3A/B-II increased in a concentration-dependent manner.
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• Cell Research:
  For transfection, A549 cells were seeded in 6-well plates to obtain 30% confluence at the time of transfection. Xtreme siRNA transfection reagent was used to transfect siRNA to a final concentration of 100 nM. Inhibition of gene expression by siRNA was determined after 48 hours by Western analysis. Cells were harvested, and the nuclear extract or total cell lysate was assayed for AP-1 DNA binding or Western blotting, respectively. HEK293T cells were cultured in complete DMEM. phCMV2-HA-MLK3 was transfected into HEK293T cells using genejammer transfection reagent using manufacturer's instructions. After 48 hours, cells were either untreated or treated with 5 or 10 μM SB202190 or SB203580 for 4 hours. Following treatment cell lysates were prepared using lysis buffer (50 mM Tris-HCl at pH 7.5, 5 mM EDTA, 150 mM NaCl, 1% Triton X-100, 50 mM NaF, 10 mM sodium pyrophosphate, 25 mM β- glycerophosphate, 1 mM PMSF, 30 μL/mL aprotinin, and 1 mM Na3VO4). 500 μg of total protein was immunoprecipitated with anti-HA-agarose conjugate. Phospho-MLK3 (Thr277/Ser281) was detected in western blotting using phosphospecific antibodies. The expression vector was transfected into HEK293T cells using Genejammer as stated earlier. After 48 hours, cell lysates was prepared and Flag-MKK7 was immunoprecipitated using anti-Flag-agarose conjugate. The Flag-MKK7 was used as a substrate for MLK3 kinase assay .
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• Animal Research:
  The pharmacological efficacy of SB-ULS-LZM was evaluated in the unilateral ischemia-reperfusion (I/R) rat model. At 2 h before the ischemia procedure, rats were injected with SB-ULS-LZM (32 mg/kg. conjugate, equivalent to 752 g/kg SB202190), vehicle (5% glucose), or free SB202190 (800 g/kg). SB-ULS-LZM was dissolved in 5% glucose, whereas SB202190 was dissolved in 20% hydroxypropyl-β-cyclodextrin solution with 5% dimethyl sulfoxide as described earlier. Compounds were administered i.v. via the penis vein as described above. Animals were allowed to recover and placed back into the cages until the induction of renal ischemia. Rats were operated, and the renal artery and vein were clamped under microscope to stop renal blood flow. After 45 min, clamps were removed, and reperfusion of the kidney was observed before closing of the wound. Sham-operated animals (n 3) received the same surgical procedure, with the exception of ischemia, and were included as a control group. After 4 days, animals were sacrificed, and blood samples were collected from the abdominal aorta. Kidneys were isolated after gently flushing the organs with saline and preserved in 4% formalin for preparation of paraffin-embedded sections or frozen in ice-cold isopentane for preparation of cryosections .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

p38α, p38β, p38MAPK, pocket, p38 MAPK, spatial, SB 202190, SB202190, SB-202190, deficits, colorectal, Autophagy, ATP, Apoptosis, anti-cancer, FHPI, Inhibitor, memory, learning, inhibit

Compound Identifiers

PubChem CID

5169