GNA002 - ≥98% , CAS No.1385035-79-9

CAS: 1385035-79-9 Cat. No.: G650478 Formula: C₄₂H₅₅NO₈ Molecular Weight: 701.89 PubChem CID: 138911304

GRADE & PURITY ≥98%

Storage

Store at -20°C,Argon charged

Shipped In

Ice chest + Ice pads

Overview

GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC 50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes

In Vitro

GNA002 (10 μM; 72 hours) clearly inhibits the proliferation of numerous cancer cell lines with IC 50 s of 0.070 μM and 0.103 μM for MV4-11 and RS4-11. GNA002 (2 μM; 24 hours) demonstrates an elevated capacity to induce cell death in human cancer cells. GNA002 (0.1-4 μM; 48 hours) efficiently reduces EZH2-mediated H3K27 trimethylation in Cal-27 head and neck cancer cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Numerous cancer cell lines Concentration: 10 μM Incubation Time: 72 hours Result: Inhibited the proliferation of numerous cancer cell lines with IC50s of 0.070 μM and 0.103 μM for MV4-11 and RS4-11. Apoptosis AnalysisCell Line: HN-4 and Cal-27 head and neck cancer cells Concentration: 2 μM Incubation Time: 24 hours Result: Induced cellular apoptosis in human cancer cells. Western Blot AnalysisCell Line: Cal-27 head and neck cancer cells Concentration: 0.1, 0.2, 0.5, 1, 2, 4 μM Incubation Time: 48 hours Result: Reduced H3K27Me3 levels.

In Vivo

GNA002 (oral administration; 100 mg/kg; daily) significantly decreases the volumes of Cal-27-derived tumors and reduces H3K27Me3 levels in tumor tissues. GNA002 also significantly suppresses the in vivo tumor growth derived from the xenografted A549 lung cancer cells, Daudi and Pfeiffer cells. GNA002 inhibits the aberrant oncogenic functions of EZH2, thus inhibiting tumor growth in vivo, at least in the xenograft experimental model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male BALB/C Nude mice aged 30-35 days and weighing 18-22 g, bearing Cal-27 xenograft tumors Dosage: 100 mg/kg Administration: Oral administration; daily Result: Decreased the size and weight of tumors formed by Cal-27 cells.

Form:Oil

IC50& Target:EZH2 1.1 μM (IC 50 )

Specifications

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC 50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of H

Storage

Store at -20°C,Argon charged

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥98%

Names and Identifiers

Canonical Smiles

CCOCCNC(=O)C(=CCC12C(=O)C3CC(C14C(=C3)C(=O)C5=C(C(=C(C(=C5O4)CC=C(C)C)O)CC=C(C)CCC=C(C)C)O)C(O2)(C)C)C

IUPAC Name

(Z)-4-[(1S,2S,13S,15R)-7-[(2E)-3,7-dimethylocta-2,6-dienyl]-6,8-dihydroxy-17,17-dimethyl-5-(3-methylbut-2-enyl)-10,14-dioxo-3,16-dioxapentacyclo[11.4.1.02,11.02,15.04,9]octadeca-4,6,8,11-tetraen-15-yl]-N-(2-ethoxyethyl)-2-methylbut-2-enamide

InChIKey

HJJVIXXMFVHPER-PTQVRNBOSA-N

INCHI

1S/C42H55NO8/c1-10-49-21-20-43-39(48)27(7)18-19-41-38(47)28-22-31-36(46)33-35(45)29(17-15-26(6)13-11-12-24(2)3)34(44)30(16-14-25(4)5)37(33)50-42(31,41)32(23-28)40(8,9)51-41/h12,14-15,18,22,28,32,44-45H,10-11,13,16-17,19-21,23H2,1-9H3,(H,43,48)/b26-15+,27-18-/t28-,32+,41+,42-/m1/s1

PubChem CID

138911304

Molecular Weight

701.89

Chemical and Physical Properties

• Solubility: DMSO : 25 mg/mL (35.62 mM; Need ultrasonic)

Frequently Asked Questions

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C under argon. It is supplied under an argon blanket; reseal under inert gas after each use.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1385035-79-9, the molecular formula is C42H55NO8, and the molecular weight is 701.89 g/mol. InChIKey HJJVIXXMFVHPER-PTQVRNBOSA-N.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.