PKM2 inhibitor 2825-0090

• CAT Number: I034859
• CAS Number: 313701-92-7
• Molecular Formula: C26H26N2O6
• Molecular Weight: 462.502
• Purity: 98%
• Synonyms: PKM2 inhibitor 2825-0090
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: 5-(2,5-Dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid; 1-(3-Carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole
• InChI: InChI=1S/2C13H13NO3/c2*1-8-3-4-9(2)14(8)10-5-6-12(15)11(7-10)13(16)17/h2*3-7,15H,1-2H3,(H,16,17)
• InChIKey: RPNDNUTUEQJRBE-UHFFFAOYSA-N
• SMILES: O=C(O)C1=CC(N2C(C)=CC=C2C)=CC=C1O.CC3=CC=C(C)N3C4=CC=C(O)C(C(O)=O)=C4

PKM2 Inhibitor 2825-0090(CAT: I034859) represents a notable compound in the field of cancer research and pharmaceutical development. As a novel pyruvate kinase M2 (PKM2) inhibitor, it holds promise for targeting cancer metabolism pathways. By inhibiting PKM2, a key enzyme involved in glycolysis and tumor growth, this compound exhibits potential in suppressing cancer progression. The observed reduction in tumor growth of non-small cell lung cancer (NSCLC) xenografts in vivo underscores its significance as a potential therapeutic agent.

Reference

1: Zhou Y, Huang Z, Su J, Li J, Zhao S, Wu L, Zhang J, He Y, Zhang G, Tao J, Zhou
J, Chen X, Peng C. Benserazide is a novel inhibitor targeting PKM2 for melanoma
treatment. Int J Cancer. 2019 Oct 25. doi: 10.1002/ijc.32756. [Epub ahead of
print] PubMed PMID: 31652354.
2: Zhou Q, Sun Y. MLN4924: additional activities beyond neddylation inhibition.
Mol Cell Oncol. 2019 May 22;6(5):e1618174. doi: 10.1080/23723556.2019.1618174.
eCollection 2019. PubMed PMID: 31528694; PubMed Central PMCID: PMC6736204.
3: Mohammad GH, Vassileva V, Acedo P, Olde Damink SWM, Malago M, Dhar DK, Pereira
SP. Targeting Pyruvate Kinase M2 and Lactate Dehydrogenase A Is an Effective
Combination Strategy for the Treatment of Pancreatic Cancer. Cancers (Basel).
2019 Sep 16;11(9). pii: E1372. doi: 10.3390/cancers11091372. PubMed PMID:
31527446; PubMed Central PMCID: PMC6770573.
4: Awasthi D, Nagarkoti S, Sadaf S, Chandra T, Kumar S, Dikshit M. Glycolysis
dependent lactate formation in neutrophils: A metabolic link between
NOX-dependent and independent NETosis. Biochim Biophys Acta Mol Basis Dis. 2019
Dec 1;1865(12):165542. doi: 10.1016/j.bbadis.2019.165542. Epub 2019 Aug 29.
PubMed PMID: 31473341.
5: Wong TL, Ng KY, Tan KV, Chan LH, Zhou L, Che N, Hoo RL, Lee TK, Richard S, Lo
CM, Man K, Khong PL, Ma S. CRAF methylation by PRMT6 regulates aerobic glycolysis
driven hepatocarcinogenesis via ERK-dependent PKM2 nuclear relocalization and
activation. Hepatology. 2019 Aug 30. doi: 10.1002/hep.30923. [Epub ahead of
print] PubMed PMID: 31469916.
6: Hsieh IS, Gopula B, Chou CC, Wu HY, Chang GD, Wu WJ, Chang CS, Chu PC, Chen
CS. Development of Novel Irreversible Pyruvate Kinase M2 Inhibitors. J Med Chem.
2019 Sep 26;62(18):8497-8510. doi: 10.1021/acs.jmedchem.9b00763. Epub 2019 Sep
16. PubMed PMID: 31465224.
7: Shen Y, Chen G, Zhuang L, Xu L, Lin J, Liu L. ARHGAP4 mediates the Warburg
effect in pancreatic cancer through the mTOR and HIF-1α signaling pathways. Onco
Targets Ther. 2019 Jun 28;12:5003-5012. doi: 10.2147/OTT.S207560. eCollection
2019. PubMed PMID: 31303760; PubMed Central PMCID: PMC6611502.
8: Macpherson JA, Theisen A, Masino L, Fets L, Driscoll PC, Encheva V, Snijders
AP, Martin SR, Kleinjung J, Barran PE, Fraternali F, Anastasiou D. Functional
cross-talk between allosteric effects of activating and inhibiting ligands
underlies PKM2 regulation. Elife. 2019 Jul 2;8. pii: e45068. doi:
10.7554/eLife.45068. PubMed PMID: 31264961; PubMed Central PMCID: PMC6636998.
9: De Rosa V, Monti M, Terlizzi C, Fonti R, Del Vecchio S, Iommelli F. Coordinate
Modulation of Glycolytic Enzymes and OXPHOS by Imatinib in BCR-ABL Driven Chronic
Myelogenous Leukemia Cells. Int J Mol Sci. 2019 Jun 27;20(13). pii: E3134. doi:
10.3390/ijms20133134. PubMed PMID: 31252559; PubMed Central PMCID: PMC6651622.
10: Liu W, Woolbright BL, Pirani K, Didde R, Abbott E, Kaushik G, Martin P,
Hamilton-Reeves J, Taylor JA 3rd, Holzbeierlein JM, Anant S, Lee EK. Tumor M2-PK:
A novel urine marker of bladder cancer. PLoS One. 2019 Jun 27;14(6):e0218737.
doi: 10.1371/journal.pone.0218737. eCollection 2019. PubMed PMID: 31246990;
PubMed Central PMCID: PMC6597081.
11: Kono M, Maeda K, Stocton-Gavanescu I, Pan W, Umeda M, Katsuyama E, Burbano C,
Orite SYK, Vukelic M, Tsokos MG, Yoshida N, Tsokos GC. Pyruvate kinase M2 is
requisite for Th1 and Th17 differentiation. JCI Insight. 2019 Jun 20;4(12). pii:
127395. doi: 10.1172/jci.insight.127395. eCollection 2019 Jun 20. PubMed PMID:
31217348; PubMed Central PMCID: PMC6629104.
12: Shin S, Kwon YJ, Ye DJ, Baek HS, Kwon TU, Kim D, Chun YJ. Human steroid
sulfatase enhances aerobic glycolysis through induction of HIF1α and glycolytic
enzymes. Biochim Biophys Acta Mol Basis Dis. 2019 Sep 1;1865(9):2464-2474. doi:
10.1016/j.bbadis.2019.06.005. Epub 2019 Jun 11. PubMed PMID: 31195119.
13: Ge XL, Wang JL, Liu X, Zhang J, Liu C, Guo L. Inhibition of miR-19a protects
neurons against ischemic stroke through modulating glucose metabolism and
neuronal apoptosis. Cell Mol Biol Lett. 2019 May 31;24:37. doi:
10.1186/s11658-019-0160-2. eCollection 2019. PubMed PMID: 31168302; PubMed
Central PMCID: PMC6545018.
14: Suzuki A, Puri S, Leland P, Puri A, Moudgil T, Fox BA, Puri RK, Joshi BH.
Subcellular compartmentalization of PKM2 identifies anti-PKM2 therapy response in
vitro and in vivo mouse model of human non-small-cell lung cancer. PLoS One. 2019
May 23;14(5):e0217131. doi: 10.1371/journal.pone.0217131. eCollection 2019.
PubMed PMID: 31120964; PubMed Central PMCID: PMC6532891.
15: Bi YH, Han WQ, Li RF, Wang YJ, Du ZS, Wang XJ, Jiang Y. Signal transducer and
activator of transcription 3 promotes the Warburg effect possibly by inducing
pyruvate kinase M2 phosphorylation in liver precancerous lesions. World J
Gastroenterol. 2019 Apr 28;25(16):1936-1949. doi: 10.3748/wjg.v25.i16.1936.
PubMed PMID: 31086462; PubMed Central PMCID: PMC6487376.
16: Beinat C, Patel CB, Xie Y, Gambhir SS. Evaluation of Glycolytic Response to
Multiple Classes of Anti-glioblastoma Drugs by Noninvasive Measurement of
Pyruvate Kinase M2 Using [(18)F]DASA-23. Mol Imaging Biol. 2019 Apr 15. doi:
10.1007/s11307-019-01353-2. [Epub ahead of print] PubMed PMID: 30989436.
17: Qi H, Ning X, Yu C, Ji X, Jin Y, McNutt MA, Yin Y. Succinylation-dependent
mitochondrial translocation of PKM2 promotes cell survival in response to
nutritional stress. Cell Death Dis. 2019 Feb 20;10(3):170. doi:
10.1038/s41419-018-1271-9. PubMed PMID: 30787272; PubMed Central PMCID:
PMC6382874.
18: Gao Y, Yang F, Yang XA, Zhang L, Yu H, Cheng X, Xu S, Pan J, Wang K, Li P.
Mitochondrial metabolism is inhibited by the HIF1α-MYC-PGC-1β axis in BRAF V600E
thyroid cancer. FEBS J. 2019 Apr;286(7):1420-1436. doi: 10.1111/febs.14786. Epub
2019 Mar 5. PubMed PMID: 30768848.
19: Ye G, Qin Y, Wang S, Pan D, Xu S, Wu C, Wang X, Wang J, Ye H, Shen H. Lamc1
promotes the Warburg effect in hepatocellular carcinoma cells by regulating PKM2
expression through AKT pathway. Cancer Biol Ther. 2019;20(5):711-719. doi:
10.1080/15384047.2018.1564558. Epub 2019 Feb 12. PubMed PMID: 30755064; PubMed
Central PMCID: PMC6605989.
20: Zhou Q, Li H, Li Y, Tan M, Fan S, Cao C, Meng F, Zhu L, Zhao L, Guan MX, Jin
H, Sun Y. Inhibiting neddylation modification alters mitochondrial morphology and
reprograms energy metabolism in cancer cells. JCI Insight. 2019 Feb 21;4(4). pii:
121582. doi: 10.1172/jci.insight.121582. eCollection 2019 Feb 21. PubMed PMID:
30668548; PubMed Central PMCID: PMC6478410.