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MedKoo Cat#: 563161 | Name: EZH2-IN-3

Description:

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

EZH2-IN-3 is an EZH2 and EZH1 inhibitor with selective impact on diffuse large B cell lymphoma cell growth.

Chemical Structure

EZH2-IN-3
EZH2-IN-3
CAS#1377997-28-8

Theoretical Analysis

MedKoo Cat#: 563161

Name: EZH2-IN-3

CAS#: 1377997-28-8

Chemical Formula: C27H28ClN5O2

Exact Mass: 489.1932

Molecular Weight: 490.00

Elemental Analysis: C, 66.18; H, 5.76; Cl, 7.23; N, 14.29; O, 6.53

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
EZH2-IN-3; EZH2 IN 3; EZH2IN3; EZH2 inhibitor 3; EZH2-inhibitor-3;
IUPAC/Chemical Name
3-Chloro-4-[2-cyano-3-(4-pyridazinyl)phenoxy]-N-(2,2,6,6-tetramethyl-4-piperidinyl)-benzamide
InChi Key
XLRMULHWFRKNQV-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H28ClN5O2/c1-26(2)13-19(14-27(3,4)33-26)32-25(34)17-8-9-24(22(28)12-17)35-23-7-5-6-20(21(23)15-29)18-10-11-30-31-16-18/h5-12,16,19,33H,13-14H2,1-4H3,(H,32,34)
SMILES Code
O=C(NC1CC(C)(C)NC(C)(C)C1)C2=CC=C(OC3=CC=CC(C4=CC=NN=C4)=C3C#N)C(Cl)=C2
Appearance
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
Shelf Life
>3 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
2934.99.03.00
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 490.00 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.

Recalculate based on batch purity %
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
1: Wang W, Lim KG, Feng M, Bao Y, Lee PL, Yu C, Chen Y, Zhang H, Marzese D, Hoon DS, Yu Q. KDM6B counteracts EZH2-mediated suppression of IGFBP5 to confer resistance to PI3K/AKT inhibitor treatment in breast cancer. Mol Cancer Ther. 2018 Jun 20. pii: molcanther.0802.2017. doi: 10.1158/1535-7163.MCT-17-0802. [Epub ahead of print] PubMed PMID: 29925528. 2: Dudakovic A, Camilleri E, Paradise CR, Samsonraj RM, Gluscevic M, Paggi CA, Begun DL, Khani F, Pichurin O, Ahmed FS, Elsayed R, Elsalanty M, McGee-Lawrence ME, Karperien M, Riester SM, Thaler R, Westendorf JJ, van Wijnen AJ. Enhancer of zeste homolog 2 (Ezh2) controls bone formation and cell cycle progression during osteogenesis in mice. J Biol Chem. 2018 Jun 13. pii: jbc.RA118.002983. doi: 10.1074/jbc.RA118.002983. [Epub ahead of print] PubMed PMID: 29899112. 3: Xu S, Xu Y, Yin M, Zhang S, Liu P, Koroleva M, Si S, Little PJ, Pelisek J, Jin ZG. Flow-dependent epigenetic regulation of IGFBP5 expression by H3K27me3 contributes to endothelial anti-inflammatory effects. Theranostics. 2018 Apr 30;8(11):3007-3021. doi: 10.7150/thno.21966. eCollection 2018. PubMed PMID: 29896299; PubMed Central PMCID: PMC5996356. 4: Daures M, Idrissou M, Judes G, Rifaï K, Penault-Llorca F, Bignon YJ, Guy L, Bernard-Gallon D. A new metabolic gene signature in prostate cancer regulated by JMJD3 and EZH2. Oncotarget. 2018 May 4;9(34):23413-23425. doi: 10.18632/oncotarget.25182. eCollection 2018 May 4. PubMed PMID: 29805743; PubMed Central PMCID: PMC5955128. 5: Li Z, Yang L, Liu X, Nie Z, Luo J. Long noncoding RNA MEG3 inhibits proliferation of chronic myeloid leukemia cells by sponging microRNA21. Biomed Pharmacother. 2018 Aug;104:181-192. doi: 10.1016/j.biopha.2018.05.047. Epub 2018 May 15. PubMed PMID: 29772439. 6: Lhuissier E, Aury-Landas J, Bouet V, Bazille C, Repesse Y, Freret T, Boumédiene K, Baugé C. Evaluation of the impact of S-adenosylmethionine-dependent methyltransferase inhibitor, 3-deazaneplanocin A, on tissue injury and cognitive function in mice. Oncotarget. 2018 Apr 17;9(29):20698-20708. doi: 10.18632/oncotarget.25062. eCollection 2018 Apr 17. PubMed PMID: 29755682; PubMed Central PMCID: PMC5945538. 7: Xi S, Payabyab EC, Straughan DM, Reardon ES, Zhang M, Hong JA, Ripley RT, Hoang CD, Schrump DS. Asbestos Induces Epigenetic Repression of Ras Association Domain-Containing Protein 1, p16 Kinase 4a Inhibitor, and p14 Alternative Reading Frame in Normal Human Mesothelial Cells. Ann Am Thorac Soc. 2018 Apr;15(Supplement_2):S123. doi: 10.1513/AnnalsATS.201707-609MG. PubMed PMID: 29676649; PubMed Central PMCID: PMC5946506. 8: Zhang P, Xiao Z, Wang S, Zhang M, Wei Y, Hang Q, Kim J, Yao F, Rodriguez-Aguayo C, Ton BN, Lee M, Wang Y, Zhou Z, Zeng L, Hu X, Lawhon SE, Siverly AN, Su X, Li J, Xie X, Cheng X, Liu LC, Chang HW, Chiang SF, Lopez-Berestein G, Sood AK, Chen J, You MJ, Sun SC, Liang H, Huang Y, Yang X, Sun D, Sun Y, Hung MC, Ma L. ZRANB1 Is an EZH2 Deubiquitinase and a Potential Therapeutic Target in Breast Cancer. Cell Rep. 2018 Apr 17;23(3):823-837. doi: 10.1016/j.celrep.2018.03.078. PubMed PMID: 29669287; PubMed Central PMCID: PMC5933875. 9: Italiano A, Soria JC, Toulmonde M, Michot JM, Lucchesi C, Varga A, Coindre JM, Blakemore SJ, Clawson A, Suttle B, McDonald AA, Woodruff M, Ribich S, Hedrick E, Keilhack H, Thomson B, Owa T, Copeland RA, Ho PTC, Ribrag V. Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study. Lancet Oncol. 2018 May;19(5):649-659. doi: 10.1016/S1470-2045(18)30145-1. Epub 2018 Apr 9. PubMed PMID: 29650362. 10: Chien YC, Liu LC, Ye HY, Wu JY, Yu YL. EZH2 promotes migration and invasion of triple-negative breast cancer cells via regulating TIMP2-MMP-2/-9 pathway. Am J Cancer Res. 2018 Mar 1;8(3):422-434. eCollection 2018. PubMed PMID: 29636998; PubMed Central PMCID: PMC5883093. 11: O'Neill KM, Irwin RE, Mackin SJ, Thursby SJ, Thakur A, Bertens C, Masala L, Loughery JEP, McArt DG, Walsh CP. Depletion of DNMT1 in differentiated human cells highlights key classes of sensitive genes and an interplay with polycomb repression. Epigenetics Chromatin. 2018 Mar 29;11(1):12. doi: 10.1186/s13072-018-0182-4. PubMed PMID: 29598829; PubMed Central PMCID: PMC5875016. 12: Bisserier M, Wajapeyee N. Mechanisms of resistance to EZH2 inhibitors in diffuse large B-cell lymphomas. Blood. 2018 May 10;131(19):2125-2137. doi: 10.1182/blood-2017-08-804344. Epub 2018 Mar 23. PubMed PMID: 29572378. 13: Pasini A, Brand OJ, Jenkins G, Knox AJ, Pang L. Suberanilohydroxamic acid prevents TGF-β1-induced COX-2 repression in human lung fibroblasts post-transcriptionally by TIA-1 downregulation. Biochim Biophys Acta. 2018 May;1861(5):463-472. doi: 10.1016/j.bbagrm.2018.03.007. Epub 2018 Mar 17. PubMed PMID: 29555582; PubMed Central PMCID: PMC5910054. 14: Lino Cardenas CL, Kessinger CW, MacDonald C, Jassar AS, Isselbacher EM, Jaffer FA, Lindsay ME. Inhibition of the methyltranferase EZH2 improves aortic performance in experimental thoracic aortic aneurysm. JCI Insight. 2018 Mar 8;3(5). pii: 97493. doi: 10.1172/jci.insight.97493. [Epub ahead of print] PubMed PMID: 29515022; PubMed Central PMCID: PMC5922285. 15: Ding H, Lu WC, Hu JC, Liu YC, Zhang CH, Lian FL, Zhang NX, Meng FW, Luo C, Chen KX. Identification and Characterizations of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Scaffold Hopping- and 2D-Molecular Fingerprint-Based Similarity Search. Molecules. 2018 Mar 2;23(3). pii: E567. doi: 10.3390/molecules23030567. PubMed PMID: 29498708. 16: Zheng S, Xiao L, Liu Y, Wang Y, Cheng L, Zhang J, Yan N, Chen D. DZNep inhibits H3K27me3 deposition and delays retinal degeneration in the rd1 mice. Cell Death Dis. 2018 Feb 22;9(3):310. doi: 10.1038/s41419-018-0349-8. PubMed PMID: 29472543; PubMed Central PMCID: PMC5833420. 17: Saito M, Saito K, Shiraishi K, Maeda D, Suzuki H, Minamiya Y, Kono K, Kohno T, Goto A. Identification of candidate responders for anti-PD-L1/PD-1 immunotherapy, Rova-T therapy, or EZH2 inhibitory therapy in small-cell lung cancer. Mol Clin Oncol. 2018 Feb;8(2):310-314. doi: 10.3892/mco.2017.1536. Epub 2017 Dec 12. PubMed PMID: 29435295; PubMed Central PMCID: PMC5776411. 18: Liu S, Liu F, Huang W, Gu L, Meng L, Ju Y, Wu Y, Li J, Liu L, Sang M. MAGE-A11 is activated through TFCP2/ZEB1 binding sites de-methylation as well as histone modification and facilitates ESCC tumor growth. Oncotarget. 2017 Dec 5;9(3):3365-3378. doi: 10.18632/oncotarget.22973. eCollection 2018 Jan 9. PubMed PMID: 29423052; PubMed Central PMCID: PMC5790469. 19: Colón-Caraballo M, Torres-Reverón A, Soto-Vargas JL, Young S, Lessey B, Mendoza A, Urrutia R, Flores I. Effects of histone methyltransferase inhibition in endometriosis. Biol Reprod. 2018 Feb 2. doi: 10.1093/biolre/ioy030. [Epub ahead of print] PubMed PMID: 29408993. 20: Hernández-Ruiz E, Toll A, García-Diez I, Andrades E, Ferrandiz-Pulido C, Masferrer E, Yébenes M, Jaka A, Gimeno J, Gimeno R, García-Patos V, Pujol RM, Hernández-Muñoz I. The Polycomb proteins RING1B and EZH2 repress the tumoral pro-inflammatory function in metastasizing primary cutaneous squamous cell carcinoma. Carcinogenesis. 2018 Mar 8;39(3):503-513. doi: 10.1093/carcin/bgy016. PubMed PMID: 29394319.