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
製品説明
IC50 & Target
|
NSD3 |
Cellular Effect
|
Cell Line
|
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] |
体外実験
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. Further protocols information, click here.
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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)