BI-9321
BI-9321, a chemical probe, is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
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- CAS 番号: 2387510-86-1
- 分子式: C22H21FN4
- 分子量:360.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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NSD3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
0.139 μM
Compound: 18; BI-9321
|
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured after 6 days in presence of JQ1 by RealTime-Glow MT cell viability assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured after 6 days in presence of JQ1 by RealTime-Glow MT cell viability assay
|
[PMID: 37182335] |
| MOLM-13 | IC50 |
26.8 μM
Compound: 18; BI-9321
|
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured after 6 days by RealTime-Glow MT cell viability assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured after 6 days by RealTime-Glow MT cell viability assay
|
[PMID: 37182335] |
| MOLM-13 | IC50 |
26.8 μM
Compound: 39; BI-9321
|
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38805937] |
| MOLM-13 | IC50 |
26.8 μM
Compound: BI-9321
|
Inhibition of cell proliferation of human MOLM-13 cells incubated for 6 days by Real-time Glow MT assay
Inhibition of cell proliferation of human MOLM-13 cells incubated for 6 days by Real-time Glow MT assay
|
[PMID: 38412693] |
BI-9321 is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 μM. As a single agent, BI-9321 downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2387510-86-1
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分子量 360.43
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分子式 C22H21FN4
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SMILES
NCC1=CC(C)=C(C2=C(C3=CC=NC4=CC(F)=CC=C34)N(C)C=N2)C(C)=C1
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)