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製品番号: 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.

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CAS 番号: 3018914-66-1
分子式: C₃₁H₃₅FN₄O₄S
分子量:578.70

保管条件:

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

Data Sheet (272 KB)

IHMT-EZH2-426 構造式

CAS 番号: 3018914-66-1

容量

価格（税別）

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数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

EZH2 WT

1.3 nM (IC₅₀)

EZH2-A687V

1.2 nM (IC₅₀)

Y641F/Y641N/Y641S

1.7-3.5 nM (IC₅₀)

Histone Methyltransferase アイソフォーム固有の製品をすべて表示 :

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]

化学情報

CAS 番号 3018914-66-1
分子量 578.70
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
化学情報
純度とドキュメンテーション
参考文献

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IHMT-EZH2-426

Histone Methyltransferase アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

IHMT-EZH2-426 関連分類

HY-156292 関連分類