SEL120-34A
Based on 8 publication(s) in Google Scholar
SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.49%
- CAS 番号: 1609522-33-9
- 分子式: C15H18Br2N4
- 分子量:414.14
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 SEL120-34A
More- Cell. 2021 Apr 15;184(8):2167-2182.e22. [Abstract]
- Blood. 2026 Feb 24:blood.2025031486. [Abstract]
- Nat Commun. 2024 Mar 19;15(1):2198. [Abstract]
- Nat Commun. 2019 Oct 18;10(1):4741. [Abstract]
- Adv Sci (Weinh). 2025 Nov 19:e18346. [Abstract]
- Int J Mol Sci. 2022 Feb 24;23(5):2493. [Abstract]
- bioRxiv. 2025 January 24.
- Friedrich-Alexander-Universität Erlangen-Nürnberg. 2023 Jun 23.
生物活性
|
CDK8/CycC 4.4 nM (IC50) |
CDK19/CycC 10.4 nM (IC50) |
CDK9/cycT 1070 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | GI50 |
5.9 μM
Compound: SEL120-34A
|
Antiproliferative activity against human A-375 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human A-375 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| A549 | GI50 |
12.06 μM
Compound: SEL120-34A
|
Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| GES1 | GI50 |
55.3 μM
Compound: SEL120-34A
|
Antiproliferative activity against human GES1 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human GES1 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| HCT-116 | GI50 |
11.3 μM
Compound: SEL120-34A
|
Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| HL-60 | GI50 |
<1000 nM
Compound: 2; SEL120-34A
|
Growth inhibition of human HL60 cells by alamar blue assay
Growth inhibition of human HL60 cells by alamar blue assay
|
[PMID: 29266937] |
| HT-29 | GI50 |
33.8 μM
Compound: SEL120-34A
|
Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| KG-1 | GI50 |
<1000 nM
Compound: 2; SEL120-34A
|
Growth inhibition of human KG1 cells by alamar blue assay
Growth inhibition of human KG1 cells by alamar blue assay
|
[PMID: 29266937] |
| MDA-MB-231 | GI50 |
9.6 μM
Compound: SEL120-34A
|
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| MGC-803 | GI50 |
16.26 μM
Compound: SEL120-34A
|
Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| MOLM-13 | GI50 |
0.02 μM
Compound: SEL120-34A
|
Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| MV4-11 | GI50 |
<1000 nM
Compound: 2; SEL120-34A
|
Growth inhibition of human MV4-11 cells by alamar blue assay
Growth inhibition of human MV4-11 cells by alamar blue assay
|
[PMID: 29266937] |
| MV4-11 | GI50 |
0.07 μM
Compound: SEL120-34A
|
Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
| MV4-11 | IC50 |
248.75 nM
Compound: RVU120; SEL120
|
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 10 days and replacement with fresh media with compounds on day 5 by CTG assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 10 days and replacement with fresh media with compounds on day 5 by CTG assay
|
[PMID: 37029334] |
| MV4-11 | IC50 |
43.77 nM
Compound: RVU120
|
Antiproliferative activity against human MV4-11 cells incubated for 5 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human MV4-11 cells incubated for 5 days by CellTiter-Glo luminescent cell viability assay
|
[PMID: 38690856] |
| OCI-AML2 | GI50 |
<1000 nM
Compound: 2; SEL120-34A
|
Growth inhibition of human OCI-AML2 cells by alamar blue assay
Growth inhibition of human OCI-AML2 cells by alamar blue assay
|
[PMID: 29266937] |
| OCI-AML-3 | GI50 |
<1000 nM
Compound: 2; SEL120-34A
|
Growth inhibition of human OCI-AML3 cells by alamar blue assay
Growth inhibition of human OCI-AML3 cells by alamar blue assay
|
[PMID: 29266937] |
| SW480 | GI50 |
17.7 μM
Compound: SEL120-34A
|
Antiproliferative activity against human SW480 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human SW480 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 36889252] |
SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively. SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). SEL120-34A is active against a panel of AML cell lines (GI50<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 1609522-33-9
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性状 Solid
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分子量 414.14
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分子式 C15H18Br2N4
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Color White to off-white
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SMILES
CC1=C2C3=C(C(Br)=C1Br)CCCN3C(N4CCNCC4)=N2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Cell
2021 Apr 15;184(8):2167-2182.e22. PMID: 33811809 -
Blood
Overcoming menin inhibitor resistance in AML cells with combinations including BET proteins and a dual BRG1/BRM inhibitor. [Abstract]2026 Feb 24:blood.2025031486. PMID: 41734382 -
Nat Commun
Oncogenic enhancers prime quiescent metastatic cells to escape NK immune surveillance by eliciting transcriptional memory. [Abstract]2024 Mar 19;15(1):2198. PMID: 38503727 -
Nat Commun
2019 Oct 18;10(1):4741. PMID: 31628323 -
Adv Sci (Weinh)
NUDT21-mediated Alternative Polyadenylation of CDK19 Reprograms Cholesterol Biosynthesis to Drive Colorectal Cancer Progression. [Abstract]2025 Nov 19:e18346. PMID: 41255211 -
Int J Mol Sci
Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]2022 Feb 24;23(5):2493. PMID: 35269635 -
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溶剤 & 溶解度
DMSO : 20 mg/mL (48.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4146 mL | 12.0732 mL | 24.1464 mL | 60.3661 mL |
| 5 mM | 0.4829 mL | 2.4146 mL | 4.8293 mL | 12.0732 mL | |
| 10 mM | 0.2415 mL | 1.2073 mL | 2.4146 mL | 6.0366 mL | |
| 15 mM | 0.1610 mL | 0.8049 mL | 1.6098 mL | 4.0244 mL | |
| 20 mM | 0.1207 mL | 0.6037 mL | 1.2073 mL | 3.0183 mL | |
| 25 mM | 0.0966 mL | 0.4829 mL | 0.9659 mL | 2.4146 mL | |
| 30 mM | 0.0805 mL | 0.4024 mL | 0.8049 mL | 2.0122 mL | |
| 40 mM | 0.0604 mL | 0.3018 mL | 0.6037 mL | 1.5092 mL |