SB 203580 A specific inhibitor of p38 activation of MK2

SB 203580 (CAS 152121-47-6)

SB 203580 | CAS 152121-47-6 is rated 5.0 out of 5 by 4.
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Synonym: PB 203580; RWJ 64809
Application: A specific inhibitor of p38 activation of MK2
CAS Number: 152121-47-6
Purity: ≥98%
Molecular Weight: 377.43
Molecular Formula: C21H16FN3OS
* Refer to Certificate of Analysis for lot specific data (including water content).
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SB 203580, a pyridinyl imidazole, has been observed to suppress p38 mediated activation of MAPKAP kinase-2 (MAPKAPK-2 or MK2), yet does not disrupt JNK activity.Mitogen-activated protein kinases (MAPK) are a group of serine and threonine-specific kinases sensitive to cellular stress, heat shock, and proinflammatory cytokines. p38 (p38 MAPK) is crucial for normal inflammatory and immune responses as it regulates the expression of varying cell surface receptors, cytokines and transcription factors. SB 203580 inhibits heat shock protein 27 (HSP 27) phosphorylation and has been shown to induce the activation of Raf-1. SB 203580 has also been shown to inhibit phosphoinositide-dependent protein kinase 1 (PKB Kinase), consequently preventing the activation of PKB/Akt. SB 203580 is a useful tool to assess the physiological roles of p38, and for deriving and maintaining embryonic stem cells. SB 203580 is an inhibitor of p38 α, p38 β, Cox-1, Cox-2, GSK, TXA Synthase and RICK.


References

1. Cuenda, A., et al. 1995. FEBS Lett. 364: 229-233. PMID: 7750577
2. Saklatvala, J., et al. 1996. J. Biol. Chem. 271: 6586-6589. PMID: 8636072
3. Young, P.R., et al. 1997. J. Biol. Chem. 272: 12116-12121. PMID: 9115281
4. Clerk, A. and Sugden, P.H. 1998. FEBS Lett. 426: 93-96. PMID: 9598985
5. Hashimoto, S., et al. 1999. Biochem. Biophys. Res. Commun. 258: 443-447. PMID: 10329406
6. Kalmes, A., et al. 1999. FEBS Lett. 444: 71-74. PMID: 10037150
7. Hall-Jackson, C.A., et al. 1999. Oncogene. 18: 2047-2054. PMID: 10321729
8. Qi, X., et al. 2004. Proc. Natl. Acad. Sci. U.S.A. 101: 6027-6032. PMID: 15075392
9. Cao, W., et al. 2006. Am. J. Physiol. Gastrointest. Liver Physiol. 291: G672-G680. PMID: 16645161

Physical State :
Solid
Solubility :
Soluble in DMSO (50 mg/ml), aqueous buffers (Sparingly soluble), methanol, acetone, ethanol (~0.2 mg/ml), and 1:9 solution of DMF:PBS(PH 7.2) (~0.5 mg/ml).
Storage :
Store at -20° C
Melting Point :
280.73° C (Predicted)
Boiling Point :
~615.6° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.71
IC50 :
p38 MAP kinase : IC50 = 34 nM; IL-1 and TNF-α : IC50 = 50-100 nM (LPS-stimulated human monocytes and the human monocyte cell line THP-1); SAPK2a/p38: EC5050 = 50 nM; SAPK2b/p38β2: IC50 = 500 nM
Ki Data :
MAP kinase p38 alpha: Ki= 18 nM (Homo sapiens); c-Jun N-terminal kinase 3: Ki= 90 nM (Homo sapiens)
pK Values :
pKb: 9.09
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
UT3967600
PubChem CID :
176155
MDL Number :
MFCD00922198
SMILES :
CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F

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SB 203580  Product Citations

See how others have used SB 203580. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 143 total

PMID: # 28753407  Hosokawa, Y. et al. 2017. Immunol. Invest. 46: 615-624.

PMID: # 28120492  Palm, E. et al. 2017. APMIS. 125: 157-169.

PMID: # 28383550  Wassermann-Dozorets, R. et al. 2017. Cell Death Dis. 8: e2733.

PMID: # 28327651  Hsieh, MJ. et al. 2017. Sci Rep. 7: 45039.

PMID: # 27896541  Hosokawa, Y. et al. 2017. Inflammation. 40: 360-365.

PMID: # 28468003  Wang, Y. et al. 2017. Cell. Physiol. Biochem. 41: 2432-2446.

PMID: # 27156806  Wang, SX. et al. 2016. Burns. 42: 1513-1521.

PMID: # 27245369  Zhang, G. et al. 2016. J. Exp. Zool. B Mol. Dev. Evol. 326: 237-49.

PMID: # 27619995  Wu, Y. et al. 2016. J. Immunol.

PMID: # 26913605  Chen, W. et al. 2016. Cell Death Dis. 7: e2115.

Citations 1 to 10 of 143 total

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. The compound, sc-3533, is provided as a white powder. If you have any further the questions or concerns, please feel free to contact our Technical Services department by calling 800-457-3801 option 2, emailing scbt@scbt.com, or using the Live Chat function on our website.
Answered by: Tech Service 8
Date published: 2017-01-17

What is the long-term storage recommendation for this product in solution with DMSO?

Asked by: two2igm05
Thank you for your question. In DMSO, it can be stored for up to 6 months without degradation at -80 degrees Celsius. Please contact Technical Service if you have further questions concerning this product.
Answered by: Tech Service 9
Date published: 2016-12-16
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Rated 5 out of 5 by from SB203580 I bough this copped to study its effects on ipsc. Im very happy with the compound performance.
Date published: 2018-03-19
Rated 5 out of 5 by from Good features! I bought it 28 months ago and boght it again 25 months ago. The inhibitive effect was very good and specific.
Date published: 2016-11-01
Rated 5 out of 5 by from The SCBT product The SCBT product, sc-3533, a p38MAPK inhibitor, was used to pre-treat HUVEC cells prior to exposure to TNF in an effort to see if TNF has an effect on genes involved in p38MAPK mediated down regulation (PubMed ID 24299952). -SCBT Publication Review
Date published: 2015-03-06
Rated 5 out of 5 by from H1299 and A549 cells were pre H1299 and A549 cells were pre-treated with sc-3533 (from SCBT) before exposure to LY2603618 to see if p38 MAPK plays a part in LY2603618 induced caspase cleavage (PubMed ID 24928205). -SCBT Publication Review
Date published: 2015-03-06
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