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Cat. No.: HY-156292

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IHMT-EZH2-426

IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC₅₀ values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.

For research use only. We do not sell to patients.

CAS No.: 3018914-66-1
Formula: C₃₁H₃₅FN₄O₄S
Molecular Weight:578.70

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

IHMT-EZH2-426 Chemical Structure

CAS No.: 3018914-66-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EZH2 WT

1.3 nM (IC₅₀)

EZH2-A687V

1.2 nM (IC₅₀)

Y641F/Y641N/Y641S

1.7-3.5 nM (IC₅₀)

All Histone Methyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Breast carcinoma cell	GI₅₀	4.79 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human 3D Triple-negative breast cancer cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human 3D Triple-negative breast cancer cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
Daudi	GI₅₀	7.01 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human Daudi cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Daudi cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
Farage	GI₅₀	>10 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human Farage cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Farage cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
KARPAS-422	GI₅₀	0.085 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human KARPAS-422 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human KARPAS-422 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
MDA-MB-231	GI₅₀	6.78 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human MDA-MB-231 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
MDA-MB-468	GI₅₀	1.93 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human MDA-MB-468 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-468 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
Pfeiffer	GI₅₀	0.02 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human Pfeiffer cells expressing A677G mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Pfeiffer cells expressing A677G mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
Raji	GI₅₀	>10 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
SUD4	GI₅₀	1.42 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human SU-DHL-4 cells expressing Y641S mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-4 cells expressing Y641S mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
SU-DHL-6	GI₅₀	1.95 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human SU-DHL-6 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-6 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
WSUDLCL2	GI₅₀	3.85 μM Compound: 38; IHMT-EZH2-426	Antiproliferative activity against human WSUDLCL2 cells expressing Y641F mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human WSUDLCL2 cells expressing Y641F mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]

Chemical Information

CAS No. 3018914-66-1
Molecular Weight 578.70
Formula C₃₁H₃₅FN₄O₄S
SMILES

O=C(C1=CC(C(C=CC(F)=C2)=C2NC(C=C)=O)=CC(N(C3CCOCC3)C)=C1C)NCC4=C(SC)C=C(C)NC4=O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Bin Zhou, et al. Discovery of dihydropyridinone derivative as a covalent EZH2 degrader. Eur J Med Chem. 2023 Oct 2:261:115825. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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IHMT-EZH2-426

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

IHMT-EZH2-426 Related Classifications

HY-156292 Related Classifications