p38 MAP Kinase Inhibitor IV
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531400

CAS#: 1638-41-1

Description: p38 MAP Kinase Inhibitor IV is an ATP-competitive inhibitor of p38α/β MAPK with IC50 values of 130 nM for p38α and 550 nM for p38β. It is much less active with ≤23% inhibition at 1 μM against p38γ/σ, ERK1/2, and JNK1/2/3. Shown to be more effective than SB 203580 in inhibiting LPS-induced IL-1β release from hPBMC (100% vs. 50% inhibition with 100 μM inhibitor). A recent study showed that p38 MAP Kinase Inhibitor IV could consistently and significantly enhance reprogramming and iPS cell generation from somatic cells.


Price and Availability

Size
Price

5mg
USD 265
Size
Price

25mg
USD 550
Size
Price

p38 MAP Kinase Inhibitor IV purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 531400
Name: p38 MAP Kinase Inhibitor IV
CAS#: 1638-41-1
Chemical Formula: C12H4Cl6O4S
Exact Mass: 453.7961
Molecular Weight: 456.92
Elemental Analysis: C, 31.54; H, 0.88; Cl, 46.55; O, 14.01; S, 7.02


Synonym: p38 MAP Kinase Inhibitor IV

IUPAC/Chemical Name: 2,2′-Sulfonyl-bis-(3,4,6-trichlorophenol)

InChi Key: AKUKHICVNCCQHN-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H4Cl6O4S/c13-3-1-5(15)9(19)11(7(3)17)23(21,22)12-8(18)4(14)2-6(16)10(12)20/h1-2,19-20H

SMILES Code: O=S(C1=C(Cl)C(Cl)=CC(Cl)=C1O)(C2=C(Cl)C(Cl)=CC(Cl)=C2O)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>3 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
2934990300


References

1: Mohetaer M, Li G, Wang Y, Cao L. Protective effects of gemigliptin against type II collagen degradation in human chondrocytes. Biomed Pharmacother. 2018 Aug;104:590-594. doi: 10.1016/j.biopha.2018.04.018. Epub 2018 May 25. PubMed PMID: 29803171.

2: Cherla R, Zhang Y, Ledbetter L, Zhang G. Coxiella burnetii Inhibits Neutrophil Apoptosis by Exploiting Survival Pathways and Antiapoptotic Protein Mcl-1. Infect Immun. 2018 Mar 22;86(4). pii: e00504-17. doi: 10.1128/IAI.00504-17. Print 2018 Apr. PubMed PMID: 29311244; PubMed Central PMCID: PMC5865014.

3: Beyfuss K, Hood DA. A systematic review of p53 regulation of oxidative stress in skeletal muscle. Redox Rep. 2018 Dec;23(1):100-117. doi: 10.1080/13510002.2017.1416773. Epub 2018 Jan 3. Review. PubMed PMID: 29298131.

4: Feng Y, Hu Y. Bone morphogenetic protein 9 serves a protective role in response to ischemic reperfusion in the brain by promoting ERK activation. Mol Med Rep. 2018 Feb;17(2):2845-2852. doi: 10.3892/mmr.2017.8253. Epub 2017 Dec 11. PubMed PMID: 29257291; PubMed Central PMCID: PMC5783498.

5: Zhang H, Zhang R, Chen J, Shi M, Li W, Zhang X. High Mobility Group Box1 Inhibitor Glycyrrhizic Acid Attenuates Kidney Injury in Streptozotocin-Induced Diabetic Rats. Kidney Blood Press Res. 2017;42(5):894-904. doi: 10.1159/000485045. Epub 2017 Nov 15. PubMed PMID: 29241180.

6: Song WJ, Dong Y, Luo C, Chen YY. p38MAPK family isoform p38α and activating transcription factor 2 are associated with the malignant phenotypes and poor prognosis of patients with ovarian adenocarcinoma. Pathol Res Pract. 2017 Oct;213(10):1282-1288. doi: 10.1016/j.prp.2017.08.003. Epub 2017 Aug 25. PubMed PMID: 28916425.

7: Yu Q, Du F, Douglas JT, Yu H, Yan SS, Yan SF. Mitochondrial Dysfunction Triggers Synaptic Deficits via Activation of p38 MAP Kinase Signaling in Differentiated Alzheimer's Disease Trans-Mitochondrial Cybrid Cells. J Alzheimers Dis. 2017;59(1):223-239. doi: 10.3233/JAD-170283. PubMed PMID: 28598851; PubMed Central PMCID: PMC5935489.

8: Aroor AR, Habibi J, Kandikattu HK, Garro-Kacher M, Barron B, Chen D, Hayden MR, Whaley-Connell A, Bender SB, Klein T, Padilla J, Sowers JR, Chandrasekar B, DeMarco VG. Dipeptidyl peptidase-4 (DPP-4) inhibition with linagliptin reduces western diet-induced myocardial TRAF3IP2 expression, inflammation and fibrosis in female mice. Cardiovasc Diabetol. 2017 May 5;16(1):61. doi: 10.1186/s12933-017-0544-4. PubMed PMID: 28476142; PubMed Central PMCID: PMC5420102.

9: Wang R, Zhang H, Wang Y, Song F, Yuan Y. Inhibitory effects of quercetin on the progression of liver fibrosis through the regulation of NF-кB/IкBα, p38 MAPK, and Bcl-2/Bax signaling. Int Immunopharmacol. 2017 Jun;47:126-133. doi: 10.1016/j.intimp.2017.03.029. Epub 2017 Apr 6. PubMed PMID: 28391159.

10: Said M, Brouard I, Quintana J, Estévez F. Antiproliferative activity and apoptosis induction by 3',4'-dibenzyloxyflavonol on human leukemia cells. Chem Biol Interact. 2017 Apr 25;268:13-23. doi: 10.1016/j.cbi.2017.02.010. Epub 2017 Feb 22. PubMed PMID: 28235426.

11: Chang YC, Chang YS, Hsieh MC, Wu HJ, Wu MH, Lin CW, Wu WC, Kao YH. All-trans retinoic acid suppresses the adhering ability of ARPE-19 cells via mitogen-activated protein kinase and focal adhesion kinase. J Pharmacol Sci. 2016 Dec;132(4):262-270. doi: 10.1016/j.jphs.2016.11.002. Epub 2016 Nov 16. PubMed PMID: 27919568.

12: Hsu CW, Li SC, Chang NY, Chen ZW, Liao JW, Chen TH, Wang JP, Lin JH, Hsuan SL. Involvement of NF-κB in regulation of Actinobacillus pleuropneumoniae exotoxin ApxI-induced proinflammatory cytokine production in porcine alveolar macrophages. Vet Microbiol. 2016 Nov 15;195:128-135. doi: 10.1016/j.vetmic.2016.09.020. Epub 2016 Sep 28. PubMed PMID: 27771058.

13: Deng W, Abliz A, Xu S, Sun R, Guo W, Shi Q, Yu J, Wang W. Severity of pancreatitis associated intestinal mucosal barrier injury is reduced following treatment with the NADPH oxidase inhibitor apocynin. Mol Med Rep. 2016 Oct;14(4):3525-34. doi: 10.3892/mmr.2016.5678. Epub 2016 Aug 26. PubMed PMID: 27573037; PubMed Central PMCID: PMC5042780.

14: Yue X, Wu M, Jiang H, Hao J, Zhao Q, Zhu Q, Saren G, Zhang Y, Zhang X. Endothelial lipase is upregulated by interleukin-6 partly via the p38 MAPK and p65 NF-κB signaling pathways. Mol Med Rep. 2016 Sep;14(3):1979-85. doi: 10.3892/mmr.2016.5457. Epub 2016 Jun 30. PubMed PMID: 27430252; PubMed Central PMCID: PMC4991746.

15: Kumar L, Yadav SK, Kushwaha B, Pandey A, Sharma V, Verma V, Maikhuri JP, Rajender S, Sharma VL, Gupta G. Energy Utilization for Survival and Fertilization-Parsimonious Quiescent Sperm Turn Extravagant on Motility Activation in Rat. Biol Reprod. 2016 Apr;94(4):96. doi: 10.1095/biolreprod.115.137752. Epub 2016 Mar 16. PubMed PMID: 26984998.

16: Sarkar J, Chowdhury A, Chakraborti T, Chakraborti S. Cross-talk between NADPH oxidase-PKCα-p(38)MAPK and NF-κB-MT1MMP in activating proMMP-2 by ET-1 in pulmonary artery smooth muscle cells. Mol Cell Biochem. 2016 Apr;415(1-2):13-28. doi: 10.1007/s11010-016-2673-6. Epub 2016 Feb 24. PubMed PMID: 26910780.

17: Christie JD, Vaslef S, Chang PK, May AK, Gunn SR, Yang S, Hardes K, Kahl L, Powley WM, Lipson DA, Bayliffe AI, Lazaar AL. A Randomized Dose-Escalation Study of the Safety and Anti-Inflammatory Activity of the p38 Mitogen-Activated Protein Kinase Inhibitor Dilmapimod in Severe Trauma Subjects at Risk for Acute Respiratory Distress Syndrome. Crit Care Med. 2015 Sep;43(9):1859-69. doi: 10.1097/CCM.0000000000001132. PubMed PMID: 26102252.

18: Zhang YY, Guo QY, Wu MY, Zang CS, Ma FZ, Sun T, Wang WN, Miao LN, Xu ZG. p16ink4a Expression Is Increased through 12-Lipoxygenase in High Glucose-Stimulated Glomerular Mesangial Cells and Type 2 Diabetic Glomeruli. Nephron. 2015;130(2):141-50. doi: 10.1159/000431106. Epub 2015 May 28. PubMed PMID: 26022507.

19: Zhou X, Wang C, Tian J, Wang Y, Li Y, Hu Z, Li R. Mitogen-activated protein kinase mediates mevalonate-stimulated human mesangial cell proliferation. Mol Med Rep. 2015 Aug;12(2):2643-9. doi: 10.3892/mmr.2015.3715. Epub 2015 May 4. PubMed PMID: 25936991; PubMed Central PMCID: PMC4464046.

20: Zhang L, Ji L, Tang X, Chen X, Li Z, Mi X, Yang L. Inhibition to DRP1 translocation can mitigate p38 MAPK-signaling pathway activation in GMC induced by hyperglycemia. Ren Fail. 2015 Jun;37(5):903-10. doi: 10.3109/0886022X.2015.1034607. Epub 2015 Apr 10. PubMed PMID: 25857570.