Molecular structure of PP242, CAS Number: 1092351-67-1
PP242 (CAS 1092351-67-1)
See product citations (8)
Alternate Names:
2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol
Application:
PP242 is a selective FRAP inhibitor
CAS Number:
1092351-67-1
Purity:
≥98%
Molecular Weight:
308.34
Molecular Formula:
C16H16N6O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
PP242 may act to be a an ATP-competitive FRAP (mTORC1/mTORC2) inhibitor (IC50 = 8 nM). PP242 is the first selective inhibitor that targets the ATP domain of FRAP. This compound shows selectivity for FRAP over other PI 3-kinase (PI 3K family kinases) (IC50 values are 0.102, 0.408, 1.27, 1.96 and 2.2 muM for p110gamma, DNA-PK, PI 3-kinase p110deltap110delta, p110alpha and p110beta respectively). Furthermore, PP242 inhibits both S6K and 4EBP1 phosphorylation this activity displays an overall decrease in cap-dependent protein translation. PP242 is an inhibitor of JAK2 and PKC alpha. PP242 is an inhibitor of JAK2, PKC alpha, PKC beta and Ret.
PP242 (CAS 1092351-67-1) References
- The PP242 mammalian target of rapamycin (mTOR) inhibitor activates extracellular signal-regulated kinase (ERK) in multiple myeloma cells via a target of rapamycin complex 1 (TORC1)/eukaryotic translation initiation factor 4E (eIF-4E)/RAF pathway and activation is a mechanism of resistance. | Hoang, B., et al. 2012. J Biol Chem. 287: 21796-805. PMID: 22556409
- Comparative effects of PP242 and rapamycin on mTOR signalling and NOTCH signalling in leukemia cells. | Ono, A., et al. 2013. Anticancer Res. 33: 809-13. PMID: 23482748
- PP242 suppresses cell proliferation, metastasis, and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway. | Xing, X., et al. 2014. Anticancer Drugs. 25: 1129-40. PMID: 25035961
- PP242 synergizes with suberoylanilide hydroxamic acid to inhibit growth of ovarian cancer cells. | Qin, Y., et al. 2014. Int J Gynecol Cancer. 24: 1373-80. PMID: 25188886
- The dual mTORC1 and mTORC2 inhibitor PP242 shows strong antitumor activity in a pheochromocytoma PC12 cell tumor model. | Zhang, X., et al. 2015. Urology. 85: 273.e1-7. PMID: 25440763
- The antileukemia roles of PP242 alone or in combination with daunorubicin in acute leukemia. | Shi, F., et al. 2015. Anticancer Drugs. 26: 410-21. PMID: 25535978
- PP242 suppresses bladder cancer cell proliferation and migration through deactivating the mammalian target of rapamycin complex 2/AKT1 signaling pathway. | Zhang, Z., et al. 2016. Mol Med Rep. 13: 333-8. PMID: 26548560
- Combination of cetuximab and PP242 synergistically suppress the progression of wild-type KRAS colorectal carcinoma. | Cheng, L., et al. 2015. Onco Targets Ther. 8: 3185-92. PMID: 26586952
- mTOR kinase inhibitor pp242 causes mitophagy terminated by apoptotic cell death in E1A-Ras transformed cells. | Gordeev, SA., et al. 2015. Oncotarget. 6: 44905-26. PMID: 26636543
- Autophagy impairment with lysosomal and mitochondrial dysfunction is an important characteristic of oxidative stress-induced senescence. | Tai, H., et al. 2017. Autophagy. 13: 99-113. PMID: 27791464
- Impact on Autophagy and Ultraviolet B Induced Responses of Treatment with the MTOR Inhibitors Rapamycin, Everolimus, Torin 1, and pp242 in Human Keratinocytes. | Xu, S., et al. 2017. Oxid Med Cell Longev. 2017: 5930639. PMID: 28400912
- PP242 Counteracts Glioblastoma Cell Proliferation, Migration, Invasiveness and Stemness Properties by Inhibiting mTORC2/AKT. | Mecca, C., et al. 2018. Front Cell Neurosci. 12: 99. PMID: 29692710
- mTOR inhibitor PP242 increases antitumor activity of sulforaphane by blocking Akt/mTOR pathway in esophageal squamous cell carcinoma. | Lu, Z., et al. 2022. Mol Biol Rep. 49: 451-461. PMID: 34731371
- Combination of mTOR inhibitor PP242 and AMPK activator metformin exerts enhanced inhibitory effects on colorectal carcinoma cells in vitro by blocking multiple kinase pathways. | Sun, C., et al. 2022. J Chemother. 1-11. PMID: 35731713
- The Role of Green Tea Catechin Epigallocatechin Gallate (EGCG) and Mammalian Target of Rapamycin (mTOR) Inhibitor PP242 (Torkinib) in the Treatment of Spinal Cord Injury. | Machova Urdzikova, L., et al. 2023. Antioxidants (Basel). 12: PMID: 36829922
Inhibitor of:
1700011E24Rik, 1700011H22Rik, 1700011L22Rik, 1700012A03Rik, 1700012B09Rik, 1700012O15Rik, 1700013G24Rik, 1700020N15Rik, 1700021C14Rik, 1700021F02Rik, 2310030G06Rik, 4E-BP1, 4E-BP2, 4E-BP3 (EIF4EBP3), 5430416O09Rik, 9430016H08Rik, A930005I04Rik, ADAL, ANKRD17, BC051070, C10orf122, C11orf35, C11orf46, C11orf71, C11orf75_BC017612, C12orf29, C14orf145, C16orf67, C19orf53, C1orf14_1700012A16Rik, C1orf210, C1orf53, C230052I12Rik, C230055K05Rik, C4orf3, Cactin, CAGE-1, CCDC102B, CCDC117, CCDC151, CCDC157, CCDC22, CCDC39, CCDC51, CCDC71, CCDC97, CECR4, Cerebellin 2, COTE1, CREBL2, D2Bwg1335e, D4Ertd196e, D9Ertd402e, DAZ1, DAZ3, DENND1A, DEPDC6, DEPTOR, EG231736, EG435337, EG546901, EIF3S6IP, EVA1B, FAM159B, FAM169B, FAM228B_A830093I24Rik, FAM23B, FOXJ3, FRBZ1, FRG2A, FYTTD1, GβL, GAP-assoc p62, GATSL2, GCN2, GIGYF2, GIMAP2, GIMAP6, Gln3, GRB10, GRRP1, HYPM, Imp3, IMPACT, IRGM, IRGM (immunity-related GTPase family M), JAK, JAK2, KIAA1609, LAMTOR4, LOC645949, LOC646864, LOC728181, LOC729639, LOC729974, LRBA, LYPD1, LYSMD1, Mam1, MGRN1, MIOS, MS4A8B, MTMR10, MTMR11, mTOR, neuroguidin, NHSL2, NumbL, OFD1, OTTMUSG00000002040, OTTMUSG00000002042, OTTMUSG00000002045, OTTMUSG00000002180, OTTMUSG00000002191, OTTMUSG00000002200, OTTMUSG00000002201, OTTMUSG00000002543, OTTMUSG00000003605, OTTMUSG00000003606, OTTMUSG00000003947, OTTMUSG00000004010, OTTMUSG00000004012, OTTMUSG00000004013, OTTMUSG00000004461, OTTMUSG00000004551, OTTMUSG00000010694, OTTMUSG00000019256, p49/STRAP, p52 S6 kinase, PHLDB3, PI 3-kinase p110 delta, Pira11, Pira2, PKC beta, PLEKHA4, PP2Cζ, PRAS40, PRLH, Protor-2, PRR14, PRR22, PRR5, PSG5, Rae-1δ, Rag A, Rag B, Rag C, RAP, REDD-2, Ret, RhebL1, Ribosomal Protein S6, RIMKLA, Ser/Thr Protein Kinase, Ser/Thr protein phosphatase (PP2C), SgK269, Sgk494, SLC38A9, SNED1, SPATA17, SSXB1, Svs3b, SZT2, Tap42, TBC1D10C, TBC1D3H, TEF-4, TINAGL1, Tip41, TLCD2, TMEM82, TOB2, Tor1, Tor2, TORC1, TORC2, TSSC1, TXR1, ULK3, V1RC15, V1RE3, Vmn1r204, WIPI-3, Ypk2, and ZPR1.Activator of:
BC030396, C330006A16Rik, dysferlin activators, E6TP1_Sipa1l1, eIF4E2, eIF4E3, Fyn, GAK, Int-6, LARP1, MIP-T3, MLSN1, MOB1A, MTMR2, NUB1, Olfr774, OXSR1, PERQ1, POLR2E, PRRT4, Rab 24, Rab 26, RB1CC1, Rictor, SMG1, SRP68, TBKBP1, WDFY1, WDFY2, and X11α.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PP242, 1 mg | sc-301606A | 1 mg | $57.00 | |||
PP242, 5 mg | sc-301606 | 5 mg | $172.00 |