2. Epigenetics Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  3. Histone Methyltransferase HSP Apoptosis
  4. EZH2/HSP90-IN-29

EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB).

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EZH2/HSP90-IN-29 Chemical Structure

EZH2/HSP90-IN-29 Chemical Structure

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EZH2/HSP90-IN-29 Related Antibodies

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Description

EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB)[1].

IC50 & Target

EZH2

6.29 nM (IC50)

HSP90

60.1 nM (IC50)

In Vitro

EZH2/HSP90-IN-29 inhibits cell proliferation against TMZ-resistant Glioblastoma (GBM) cell lines (with an IC50 of 1.015 μM) through modulation of EZH2 and HSP90 chaperone in a balanced manner[1].
EZH2/HSP90-IN-29 (5 μM) decreases centromere proteins (CENPs), CDK1 and cyclin B1, which regulates the kinetochore assembly and mitosis, arrests cell cycle at M phase[1].
EZH2/HSP90-IN-29 (2 μM) inhibits DNA repair capacity through downregulations of gene expreesions of RB Binding Protein (RBBP8), BRCA1, DNA repair and recombination protein RAD54B, RAD21, crossover junction endonuclease EME1 and BRIP1 in Pt3R cells[1].
EZH2/HSP90-IN-29 (5 μM) upregulates levels of ROS and cleaved caspase-3, increased mitochondria-derived ROS [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EZH2/HSP90-IN-29 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: Pt3R
Concentration: 0-50 μM
Incubation Time: 72 h
Result: Inhibited 50% cell viability with concentration of 1.015 μM.

Western Blot Analysis[1]

Cell Line: Pt3 and Pt3R
Concentration: 0-5 μM
Incubation Time: 72 h
Result: Decreased expressions of CDK1 and cyclin B1, increased cleaved caspase-3.
In Vivo

EZH2/HSP90-IN-29 (20 mg/kg,i.p., twice a week for 40 days) inhibited Pt3R induced tumor growth in Pt3R xenograft NOD.CB17-Prkdcscid/NCrCrl mice [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pt3R xenograft NOD.CB17-Prkdcscid/NCrCrl mice[1]
Dosage: 10-20 mg/kg
Administration: i.p., twice a week for 40 days
Result: Inhibited tumor growth.
Molecular Weight

680.83

Formula

C40H48N4O6
SMILES

O=C(NCC1=C(C=C(NC1=O)C)C)C2=CC(C3=CC=CC(N(C(C4=CC(C(C)C)=C(C=C4O)O)=O)C)=C3)=CC(N(C5CCOCC5)CC)=C2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EZH2/HSP90-IN-29 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EZH2/HSP90-IN-29Histone MethyltransferaseHSPApoptosisHeat shock proteinsPt3-RGBMCENPsInhibitorinhibitorinhibit

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