CAS No. : 1092351-67-1

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000380
Molecular Formula:C₁₆H₁₆N₆O
Molecular Weight:308.34
IC50:8 nM
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Appearance:Solid powder
Purity: > 98%
Cat No:I000380
Cas No:1092351-67-1
MDL No:MFCD12196869

PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively; also showed slightly weaker activity against BRD4 (Kd= 1.7 uM).
IC50 value: 8 nM
Target: mTOR
in vitro: PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively. PP242 displays some inhibitory activity against Ret, PKCα, PKCβ, and JAK2, while exhibits remarkable selectivity against 215 other protein kinases. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2. In BT549 cells, PP242 treatment (0.04-10 μM) inhibits the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner [1]. The p38 inhibitor SB-202190 and the PI3K inhibitor PP-242 showed slightly weaker activity (Kd values: 3.4 ± 0.13 μM and 1.7 ± 0.076 μM, respectively) [2]. PP242 potently inhibits PKCα with IC50 of 49 nM. Low concentrations of PP242 inhibit the phosphorylation of Akt S473 and higher concentrations partially inhibit Akt T308-P in addition to S473-P. As PP242 is a more effective mTORC1 inhibitor than rapamycin, PP242 inhibits the proliferation of primary MEFs, and the phosphorylation of 4EBP1 at T36/45 and S65, more potently than rapamycin. PP242 but not rapamycin potently inhibits cap-dependent translation, by causing a higher level of binding between 4EBP1 and eIF4E than rapamycin [3].
in vivo: Administration of PP242 is able to completely inhibit the phosphorylation of Akt at S473 and T308 in fat and liver of mice. PP242 only partially inhibits the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite able to fully inhibit the phosphorylation of 4EBP1 and S6 [3]. PP242 treatment potently inhibits the growth of 8226 cells in mice [4].

1:TAK-242 treatment ameliorates liver ischemia/reperfusion injury by inhibiting TLR4 signaling pathway in a swine model of Maastricht-category-III cardiac death. Shao Z, Jiao B, Liu T, Cheng Y, Liu H, Liu Y.Biomed Pharmacother. 2016 Dec;84:495-501. doi: 10.1016/j.biopha.2016.09.036. Epub 2016 Sep 28. PMID: 27685793
2:TAK-242, a Toll-Like Receptor 4 Antagonist, Protects against Aldosterone-Induced Cardiac and Renal Injury. Zhang Y, Peng W, Ao X, Dai H, Yuan L, Huang X, Zhou Q.PLoS One. 2015 Nov 10;10(11):e0142456. doi: 10.1371/journal.pone.0142456. eCollection 2015. PMID: 26556241 Free PMC Article
3:Miguel García-Sancho: Biology, computing, and the history of molecular sequencing: from proteins to DNA, 1945-2000 : Palgrave Macmillan, Basingstoke, 2012, xiii + 242 pp, illus., £55.00. Yi D.Hist Philos Life Sci. 2014 Aug;36(1):131-2. doi: 10.1007/s40656-014-0011-4. No abstract available. PMID: 26634356
4:Toll-like receptor 4 inhibitor TAK-242 treatment does not influence perfusion recovery in tissue ischemia. van den Borne P, Bastiaansen AJ, de Vries MR, Quax PH, Hoefer IE, Pasterkamp G.J Cardiovasc Pharmacol. 2014 Jan;63(1):16-22. doi: 10.1097/FJC.0000000000000019. PMID: 24084220
5:TAK-242 can be the potential agents for preventing invasion and metastasis of hepatocellular carcinoma. Yu P, Cheng X, Du Y, Huang L, Dong R.Med Hypotheses. 2013 Oct;81(4):653-5. doi: 10.1016/j.mehy.2013.06.034. Epub 2013 Jul 30. PMID: 23910073
6:Validating the incidence of coagulopathy and disseminated intravascular coagulation in patients with traumatic brain injury--analysis of 242 cases. Sun Y, Wang J, Wu X, Xi C, Gai Y, Liu H, Yuan Q, Wang E, Gao L, Hu J, Zhou L.Br J Neurosurg. 2011 Jun;25(3):363-8. doi: 10.3109/02688697.2011.552650. Epub 2011 Feb 28. PMID: 21355766
7:Morbidity and mortality in the surgical treatment of 10,242 adults with spondylolisthesis. Sansur CA, Reames DL, Smith JS, Hamilton DK, Berven SH, Broadstone PA, Choma TJ, Goytan MJ, Noordeen HH, Knapp DR Jr, Hart RA, Zeller RD, Donaldson WF 3rd, Polly DW Jr, Perra JH, Boachie-Adjei O, Shaffrey CI.J Neurosurg Spine. 2010 Nov;13(5):589-93. doi: 10.3171/2010.5.SPINE09529. PMID: 21039149
8:Amino acid substitutions at positions 242, 255 and 268 in rabies virus glycoprotein affect spread of viral infection. Ito Y, Ito N, Saito S, Masatani T, Nakagawa K, Atoji Y, Sugiyama M.Microbiol Immunol. 2010 Feb;54(2):89-97. doi: 10.1111/j.1348-0421.2009.00192.x. PMID: 20377742 Free Article
9:The novel selective toll-like receptor 4 signal transduction inhibitor tak-242 prevents endotoxaemia in conscious Guinea-pigs. Kuno M, Nemoto K, Ninomiya N, Inagaki E, Kubota M, Matsumoto T, Yokota H.Clin Exp Pharmacol Physiol. 2009 May;36(5-6):589-93. doi: 10.1111/j.1440-1681.2008.05121.x. Epub 2008 Oct 27. PMID: 19673945
10:Therapeutic effects of TAK-242, a novel selective Toll-like receptor 4 signal transduction inhibitor, in mouse endotoxin shock model. Sha T, Sunamoto M, Kitazaki T, Sato J, Ii M, Iizawa Y.Eur J Pharmacol. 2007 Oct 1;571(2-3):231-9. Epub 2007 Jun 29. PMID: 17632100
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