2. Epigenetics
  3. Histone Methyltransferase
  4. 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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IHMT-EZH2-426

IHMT-EZH2-426 構造式

CAS 番号 : 3018914-66-1

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IHMT-EZH2-426 関連抗体

Top Publications Citing Use of Products

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

すべてのアイソフォームを表示
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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.

IC50 & Target[1]

EZH2 WT

1.3 nM (IC50)

EZH2-A687V

1.2 nM (IC50)

Y641F/Y641N/Y641S

1.7-3.5 nM (IC50)

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]
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]
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]
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]
分子量

578.70

分子式

C31H35FN4O4S
CAS 番号
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
参考文献
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IHMT-EZH2-426 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:

IHMT-EZH2-4263018914-66-1Histone MethyltransferaseY641FY641NY641Sand A687Vcovalent EZH2 degraderantiproliferation effectsH3K27me3Inhibitorinhibitorinhibit

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製品名:
IHMT-EZH2-426
製品番号:
HY-156292
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