For research use only. Not for therapeutic Use.
PP242（Cat No.:I000380）is a potent and selective inhibitor of mTOR (mechanistic target of rapamycin), targeting both mTORC1 and mTORC2 complexes. Unlike rapamycin, which only partially inhibits mTORC1, PP242 effectively blocks both complexes, leading to complete suppression of downstream signaling pathways, including Akt, S6K, and 4E-BP1. This results in reduced cell growth, proliferation, and protein synthesis while promoting autophagy. PP242 is widely used in cancer research to study the impact of mTOR inhibition on tumor growth and survival, as well as in understanding mTOR’s role in various physiological and pathological processes.
| Catalog Number | I000380 |
| CAS Number | 1092351-67-1 |
| Synonyms | (2E)-2-(4-amino-1-propan-2-yl-2H-pyrazolo[3,4-d]pyrimidin-3-ylidene)indol-5-ol |
| Molecular Formula | C₁₆H₁₆N₆O |
| Purity | ≥95% |
| Target | mTOR |
| Solubility | DMSO ≥60mg/mL Water <1.2mg/mL Ethanol ≥30mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 8 nM |
| IUPAC Name | 2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol |
| InChI | InChI=1S/C16H16N6O/c1-8(2)22-16-13(15(17)18-7-19-16)14(21-22)12-6-9-5-10(23)3-4-11(9)20-12/h3-8,20,23H,1-2H3,(H2,17,18,19) |
| InChIKey | MFAQYJIYDMLAIM-UHFFFAOYSA-N |
| SMILES | CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N |
| Reference | </br>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 </br>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</br>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 </br>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 </br>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 </br>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 </br>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 </br>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</br>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 </br>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 |
