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SB 202190

Catalog No. T2301   CAS 152121-30-7
Synonyms: FHPI, SB202190

SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.

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SB 202190 Chemical Structure
SB 202190, CAS 152121-30-7
Pack Size Availability Price/USD Quantity
25 mg In stock
$ 35.00
$ 28.00
50 mg In stock
$ 50.00
$ 40.00
100 mg In stock
$ 87.00
$ 69.60
200 mg In stock
$ 163.00
$ 130.40
1 mL * 10 mM (in DMSO) In stock
$ 50.00
$ 40.00
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Purity: 99.84%
Purity: 99.73%
Purity: 99.67%
Purity: 99.66%
Purity: 99.55%
Purity: 99.21%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.
Targets&IC50 p38β:100 nM (cell free), p38α:50 nM (cell free)
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. [1]
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. [2]
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. [3]
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. [4]
Kinase Assay All protein kinase activities were linear with respect to time in every incubation. Assays were performed either manually for 10 min at 30 °C in 50 μl incubations using [γ-32P]ATP or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 min at ambient temperature in 25 μl incubations using [γ-32P]ATP. The concentrations of ATP and magnesium acetate were 0.1 mM and 10 mM respectively, unless stated otherwise. This concentration of ATP is 5–10-fold higher than the Km for ATP of most of the protein kinases studied in the present paper, but lower than the normal intracellular concentration, which is in the millimolar range. All assays were initiated with MgATP. Manual assays were terminated by spotting aliquots of each incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays were terminated by the addition of 5 μl of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers were then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity [1].
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 [3].
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 [2].
Synonyms FHPI, SB202190
Molecular Weight 331.34
Formula C20H14FN3O
CAS No. 152121-30-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33.1 mg/mL (100 mM)

TargetMolReferences and Literature

1. Nassar K, et al. A p38 MAPK inhibitor improves outcome after glaucoma filtration surgery. J Glaucoma. 2015 Feb;24(2):165-78. 2. Schwartz M, et al. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. Oncotarget. 2018 May 1;9(33):23149-23163. 3. Peng T, et al. Inhibition of p38 MAPK decreases myocardial TNF-alpha expression and improves myocardial function and survival in endotoxemia. Cardiovasc Res. 2003 Oct 1;59(4):893-900. 4. Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56. 5. Yang S, et al. Protective effects of p38 MAPK inhibitor SB202190 against hippocampal apoptosis and spatial learning and memory deficits in a rat model of vascular dementia. Biomed Res Int. 2013;2013:215798. 6. Yang C W, Hsu H Y, Chang H Y, et al. Natural cardenolides suppress coronaviral replication by downregulating JAK1 via a Na+/K+-ATPase independent proteolysis[J]. Biochemical Pharmacology. 2020: 114122.

TargetMolCitations

1. Yang S, Yang S, Zhang H, et al. Targeting Na+/K+‐ATPase by berbamine and ouabain synergizes with sorafenib to inhibit hepatocellular carcinoma. British Journal of Pharmacology. 2021 2. Chen H, He A, Li H, et al. TSSK4 upregulation in alveolar epithelial type-II cells facilitates pulmonary fibrosis through HSP90-AKT signaling restriction and AT-II apoptosis. Cell Death & Disease. 2021, 12(10): 1-1 3. Hu H, Jiang H, Zhang K, et al. Memantine nitrate MN-08 suppresses NLRP3 inflammasome activation to protect against sepsis-induced acute lung injury in mice. Biomedicine & Pharmacotherapy. 2022, 156: 113804 4. Yang C W, Hsu H Y, Chang H Y, et al. Natural cardenolides suppress coronaviral replication by downregulating JAK1 via a Na+/K+-ATPase independent proteolysis. Biochemical Pharmacology. 2020: 114122. 5. Zou X, Zeng M, Zheng Y, et al.Comparative Study of Hydroxytyrosol Acetate and Hydroxytyrosol in Activating Phase II Enzymes.Antioxidants.2023, 12(10): 1834. 6. Ouyang P, Tao Y, Wei W, et al.Spring Viremia of Carp Virus Infection Induces Carp IL-10 Expression, Both In Vitro and In Vivo.Microorganisms.2023, 11(11): 2812. 7. Feng L, Wang C, Zhang C, et al.p38 MAPK inhibitor SB202190 suppresses ferroptosis in the glutamate-induced retinal excitotoxicity glaucoma model.Neural Regeneration Research.10.4103.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Kinase Inhibitor Library Inhibitor Library Autophagy Compound Library Fluorochemical Library Anti-Colorectal Cancer Compound Library Anti-Prostate Cancer Compound Library Immunology/Inflammation Compound Library Cytoskeletal Signaling Pathway Compound Library Neural Regeneration Compound Library

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Keywords

SB 202190 152121-30-7 Apoptosis Autophagy MAPK p38 MAPK colorectal inhibit Inhibitor memory ATP anti-cancer learning SB-202190 FHPI SB202190 pocket spatial deficits inhibitor

 

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