EPZ028862

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

MedKoo CAT#: 564614

CAS#: 1887082-53-2

Description: EPZ028862 is a potent and selective SMYD3 inhibitor.


Chemical Structure

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EPZ028862
CAS# 1887082-53-2

Theoretical Analysis

MedKoo Cat#: 564614
Name: EPZ028862
CAS#: 1887082-53-2
Chemical Formula: C20H30N4O4S
Exact Mass: 422.20
Molecular Weight: 422.540
Elemental Analysis: C, 56.85; H, 7.16; N, 13.26; O, 15.15; S, 7.59

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: EPZ-028862; EPZ 028862; EPZ028862

IUPAC/Chemical Name: N-[(1R,5S)-8-(4-Aminocyclohexyl)sulfonyl-8-azabicyclo[3.2.1]octan-3-yl]-5-cyclopropyl-1,2-oxazole-3-carboxamide

InChi Key: JYZQPJRVTADXNE-MSJJKYGJSA-N

InChi Code: InChI=1S/C20H30N4O4S/c21-13-3-7-17(8-4-13)29(26,27)24-15-5-6-16(24)10-14(9-15)22-20(25)18-11-19(28-23-18)12-1-2-12/h11-17H,1-10,21H2,(H,22,25)/t13?,14?,15-,16+,17?

SMILES Code: O=C(C1=NOC(C2CC2)=C1)NC3C[C@@](N4S(=O)(C5CCC(N)CC5)=O)([H])CC[C@@]4([H])C3

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: SMYD3 has also been implicated in a number of human cancers. This enzyme is highly expressed in breast, liver, and colorectal- cancers. Knockdown of SMYD3 by RNAi has been reported to result in decreased cell proliferation in hepatocellular carcinoma, breast, cervical and esophageal cell lines and also in oncogenic KRAS -driven pancreatic cancer and lung adenocarcinoma cell lines

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 422.54 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA. Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation. PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018. PubMed PMID: 29856759; PubMed Central PMCID: PMC5983452.