PD-169316 | CAS#152121-53-4 | p38 MAPK inhibitor

MedKoo Cat#: 510236 | Name: PD-169316

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PD-169316 is a selective inhibitor of p38 MAPK. It inhibits p38 MAPK with an IC50 of 89 nM. PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells.

Chemical Structure

PD-169316

CAS#152121-53-4

Theoretical Analysis

MedKoo Cat#: 510236

Name: PD-169316

CAS#: 152121-53-4

Chemical Formula: C20H13FN4O2

Exact Mass: 360.1023

Molecular Weight: 360.35

Elemental Analysis: C, 66.66; H, 3.64; F, 5.27; N, 15.55; O, 8.88

Price and Availability

Size	Price	Availability
50mg	USD 250.00	2 Weeks
100mg	USD 450.00	2 Weeks
200mg	USD 750.00	2 Weeks
500mg	USD 1,650.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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Synonym

PD-169316; PD 169316; PD169316.

IUPAC/Chemical Name

4-(5-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-4-yl)pyridine

InChi Key

BGIYKDUASORTBB-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H13FN4O2/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(8-4-15)25(26)27/h1-12H,(H,23,24)

SMILES Code

O=[N+](C1=CC=C(C2=NC(C3=CC=NC=C3)=C(C4=CC=C(F)C=C4)N2)C=C1)[O-]

Appearance

white 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, not in water

Shelf Life

>2 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).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM.

In vitro activity:

This study shows that another p38 MAPK inhibitor, PD169316, abrogates signaling initiated by both TGFbeta and Activin A, but not bone morphogenetic protein (BMP) 4. Inhibition of TGFbeta signaling is dose dependent and results in reduced Smad2 and Smad3 phosphorylation, nuclear translocation, and up-regulation of the TGFbeta target gene Smad7. Reduced TGFbeta signaling is not due to abrogation of p38 MAPK activity, since blocking p38 MAPK activity with a dominant negative form of p38 MAPK has no effect on TGFbeta/Smad signaling. Reference: Biochem Biophys Res Commun. 2003 Oct 17;310(2):391-7. https://pubmed.ncbi.nlm.nih.gov/14521923/

In vivo activity:

Based on the strong anti-EV71 replication ability and the anti-apoptotic ability that PD169316 exhibited in vitro, this study next investigated its protective effect in an EV71-challenged suckling mouse model. Regarding the mortality of the challenged mice, PD169316 injection showed better protection (70%), as the DMSO-treated group exhibited 40% survival (Fig. 4B), but larger studies are required for a significant difference in the survival rate between the two groups. According to these results, PD169316 effectively alleviated EV71-induced illness in vivo. Reference: Virology. 2017 Aug;508:150-158. https://pubmed.ncbi.nlm.nih.gov/28545002/

	Solvent	mg/mL	mM
Solubility
	DMF	2.0	5.55
	DMF:PBS (pH 7.2) (1:2)	0.3	0.69
	DMSO	9.5	26.36

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 360.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Hu W, Lu H, Wang S, Yin W, Liu X, Dong L, Chiu R, Shen L, Lu WJ, Lan F. Suppression of Nestin reveals a critical role for p38-EGFR pathway in neural progenitor cell proliferation. Oncotarget. 2016 Dec 27;7(52):87052-87063. doi: 10.18632/oncotarget.13498. PMID: 27894083; PMCID: PMC5349970. 2. Fu Y, O'Connor LM, Shepherd TG, Nachtigal MW. The p38 MAPK inhibitor, PD169316, inhibits transforming growth factor beta-induced Smad signaling in human ovarian cancer cells. Biochem Biophys Res Commun. 2003 Oct 17;310(2):391-7. doi: 10.1016/j.bbrc.2003.09.021. PMID: 14521923. 3. Zhang Z, Wang B, Wu S, Wen Y, Wang X, Song X, Zhang J, Hou L, Chen W. PD169316, a specific p38 inhibitor, shows antiviral activity against Enterovirus71. Virology. 2017 Aug;508:150-158. doi: 10.1016/j.virol.2017.05.012. Epub 2017 May 22. PMID: 28545002.

In vitro protocol:

In vivo protocol:

1. Zhang Z, Wang B, Wu S, Wen Y, Wang X, Song X, Zhang J, Hou L, Chen W. PD169316, a specific p38 inhibitor, shows antiviral activity against Enterovirus71. Virology. 2017 Aug;508:150-158. doi: 10.1016/j.virol.2017.05.012. Epub 2017 May 22. PMID: 28545002.

1: Bahlmann LC, Xue C, Chin AA, Skirzynska A, Lu J, Thériault B, Uehling D, Yerofeyeva Y, Peters R, Liu K, Chen J, Martel AL, Yaffe M, Al-Awar R, Goswami RS, Ylanko J, Andrews DW, Kuruvilla J, Laister RC, Shoichet MS. Targeting tumour-associated macrophages in hodgkin lymphoma using engineered extracellular matrix-mimicking cryogels. Biomaterials. 2023 Jun;297:122121. doi: 10.1016/j.biomaterials.2023.122121. Epub 2023 Apr 9. PMID: 37075613. 2: Rodrigues ACBDC, Bomfim LM, Neves SP, Soares MBP, Dias RB, Valverde LF, Rocha CAG, Costa EV, da Silva FMA, Rocha WC, Koolen HHF, Bezerra DP. Tingenone and 22-hydroxytingenone target oxidative stress through downregulation of thioredoxin, leading to DNA double-strand break and JNK/p38-mediated apoptosis in acute myeloid leukemia HL-60 cells. Biomed Pharmacother. 2021 Oct;142:112034. doi: 10.1016/j.biopha.2021.112034. Epub 2021 Aug 16. PMID: 34411914. 3: Faway E, Cambier L, De Vuyst E, Evrard C, Thiry M, Lambert de Rouvroit C, Mignon B, Poumay Y. Responses of Reconstructed Human Epidermis to Trichophyton rubrum Infection and Impairment of Infection by the Inhibitor PD169316. J Invest Dermatol. 2019 Oct;139(10):2080-2089.e6. doi: 10.1016/j.jid.2019.03.1147. Epub 2019 Apr 12. PMID: 30986374. 4: Shigiyama F, Hamanoue M, Kobayashi M, Takamatsu K. Cell-permeable p38 MAP kinase protects adult hippocampal neurons from cell death. Neurosci Lett. 2019 Apr 23;699:115-121. doi: 10.1016/j.neulet.2019.02.002. Epub 2019 Feb 5. PMID: 30735722. 5: Oliveira MS, Barbosa MIF, de Souza TB, Moreira DRM, Martins FT, Villarreal W, Machado RP, Doriguetto AC, Soares MBP, Bezerra DP. A novel platinum complex containing a piplartine derivative exhibits enhanced cytotoxicity, causes oxidative stress and triggers apoptotic cell death by ERK/p38 pathway in human acute promyelocytic leukemia HL-60 cells. Redox Biol. 2019 Jan;20:182-194. doi: 10.1016/j.redox.2018.10.006. Epub 2018 Oct 12. PMID: 30359932; PMCID: PMC6198128. 6: Reddy GS, Mukhopadhyay AG, Dey CS. The p38 MAP kinase inhibitor, PD 169316, inhibits flagellar motility in Leishmania donovani. Biochem Biophys Res Commun. 2017 Dec 2;493(4):1425-1429. doi: 10.1016/j.bbrc.2017.09.135. Epub 2017 Sep 27. PMID: 28958943. 7: Leestemaker Y, de Jong A, Witting KF, Penning R, Schuurman K, Rodenko B, Zaal EA, van de Kooij B, Laufer S, Heck AJR, Borst J, Scheper W, Berkers CR, Ovaa H. Proteasome Activation by Small Molecules. Cell Chem Biol. 2017 Jun 22;24(6):725-736.e7. doi: 10.1016/j.chembiol.2017.05.010. Epub 2017 May 25. PMID: 28552582. 8: Zhang Z, Wang B, Wu S, Wen Y, Wang X, Song X, Zhang J, Hou L, Chen W. PD169316, a specific p38 inhibitor, shows antiviral activity against Enterovirus71. Virology. 2017 Aug;508:150-158. doi: 10.1016/j.virol.2017.05.012. Epub 2017 May 22. PMID: 28545002. 9: Hu W, Lu H, Wang S, Yin W, Liu X, Dong L, Chiu R, Shen L, Lu WJ, Lan F. Suppression of Nestin reveals a critical role for p38-EGFR pathway in neural progenitor cell proliferation. Oncotarget. 2016 Dec 27;7(52):87052-87063. doi: 10.18632/oncotarget.13498. PMID: 27894083; PMCID: PMC5349970. 10: Yan F, Liao R, Farhan M, Wang T, Chen J, Wang Z, Little PJ, Zheng W. Elucidating the role of the FoxO3a transcription factor in the IGF-1-induced migration and invasion of uveal melanoma cancer cells. Biomed Pharmacother. 2016 Dec;84:1538-1550. doi: 10.1016/j.biopha.2016.11.027. Epub 2016 Nov 20. PMID: 27881235. 11: Xiao C, Zhong L, Shan Z, Xu T, Gan L, Song H, Yang R, Li L, Liu B. NLS-RARα Inhibits the Effects of All-trans Retinoic Acid on NB4 Cells by Interacting with P38α MAPK. Int J Med Sci. 2016 Jul 18;13(8):611-9. doi: 10.7150/ijms.15374. PMID: 27499693; PMCID: PMC4974909. 12: Zhou X, Liu R, Duan S, Huang G, Ye Y, Kong Y. High Glucose Enhances oxLDL- Induced Apoptosis in Human Renal Proximal Tubular Epithelial Cells Largely via Inducing Lectin-Like ox-LDL Receptor-1. Pharmacology. 2016;98(1-2):20-8. doi: 10.1159/000444934. Epub 2016 Mar 23. PMID: 27003929. 13: Haines JD, Fulton DL, Richard S, Almazan G. p38 Mitogen-Activated Protein Kinase Pathway Regulates Genes during Proliferation and Differentiation in Oligodendrocytes. PLoS One. 2015 Dec 29;10(12):e0145843. doi: 10.1371/journal.pone.0145843. PMID: 26714323; PMCID: PMC4699908. 14: Mannangatti P, NarasimhaNaidu K, Damaj MI, Ramamoorthy S, Jayanthi LD. A Role for p38 Mitogen-activated Protein Kinase-mediated Threonine 30-dependent Norepinephrine Transporter Regulation in Cocaine Sensitization and Conditioned Place Preference. J Biol Chem. 2015 Apr 24;290(17):10814-27. doi: 10.1074/jbc.M114.612192. Epub 2015 Feb 27. PMID: 25724654; PMCID: PMC4409246. 15: Urriola-Muñoz P, Lagos-Cabré R, Moreno RD. A mechanism of male germ cell apoptosis induced by bisphenol-A and nonylphenol involving ADAM17 and p38 MAPK activation. PLoS One. 2014 Dec 4;9(12):e113793. doi: 10.1371/journal.pone.0113793. PMID: 25474107; PMCID: PMC4256297. 16: Cindrova-Davies T, van Patot MT, Gardner L, Jauniaux E, Burton GJ, Charnock- Jones DS. Energy status and HIF signalling in chorionic villi show no evidence of hypoxic stress during human early placental development. Mol Hum Reprod. 2015 Mar;21(3):296-308. doi: 10.1093/molehr/gau105. Epub 2014 Nov 11. PMID: 25391298; PMCID: PMC4339857. 17: Lee HS, Park EJ, Oh JH, Moon G, Hwang MS, Kim SY, Shin MK, Koh YH, Suh JH, Kang HS, Jeon JH, Rhee GS, Hong JH. Bisphenol A exerts estrogenic effects by modulating CDK1/2 and p38 MAP kinase activity. Biosci Biotechnol Biochem. 2014;78(8):1371-5. doi: 10.1080/09168451.2014.921557. Epub 2014 Jun 12. PMID: 25130739. 18: Zhong X, Wang H, Huang S. Endothelin-1 induces interleukin-18 expression in human osteoblasts. Arch Oral Biol. 2014 Mar;59(3):289-96. doi: 10.1016/j.archoralbio.2013.11.006. Epub 2013 Nov 18. PMID: 24581851. 19: Vandomme J, Touil Y, Ostyn P, Olejnik C, Flamenco P, El Machhour R, Segard P, Masselot B, Bailliez Y, Formstecher P, Polakowska R. Insulin-like growth factor 1 receptor and p38 mitogen-activated protein kinase signals inversely regulate signal transducer and activator of transcription 3 activity to control human dental pulp stem cell quiescence, propagation, and differentiation. Stem Cells Dev. 2014 Apr 15;23(8):839-51. doi: 10.1089/scd.2013.0400. Epub 2014 Jan 17. PMID: 24266654; PMCID: PMC3992006. 20: Matsuzawa T, Fujiwara E, Washi Y. Autophagy activation by interferon-γ via the p38 mitogen-activated protein kinase signalling pathway is involved in macrophage bactericidal activity. Immunology. 2014 Jan;141(1):61-9. doi: 10.1111/imm.12168. PMID: 24032631; PMCID: PMC3893850.