LL-K9-3
Based on 1 Customer Validation
LL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC50 values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer.
(Pink: CDK9/cyclinT1 ligand (HY-10008); Blue: hydrophobic tag ligand (HY-W093149); Black: linker).
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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 : 98.90%
- CAS 番号: 2809353-52-2
- 分子式: C31H49N5O6S3
- 分子量:683.95
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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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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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
CDK9 662 nM (DC50) |
cyclin T1 589 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CWR22R | IC50 |
0.095 μM
Compound: LL-K9-3
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Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay
Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay
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[PMID: 35925880] |
体外実験
LL-K9-3 (3 μM; 1-48 h) induces synchronous, time-dependent degradation of CDK9 and Cyclin T1 in 22RV1 cells, with a significant reduction starting at 5-7 h and near-complete depletion observed by 48 h[1].
LL-K9-3 (5 days) potently inhibits the proliferation of 22RV1 cells, with IC50 values of 95 nM (Ref. 1) and 224.85 nM (Ref. 2)[1][2].
LL-K9-3 (100-400 nM; 14 days) potently inhibits colony formation of 22RV1 cells at nanomolar concentrations[1].
LL-K9-3 (0.3-1 μM; 24 h) inhibits CDK9 and AR downstream signaling pathways in 22RV1 cells, including reducing the levels of cMyc, MCL-1, AR and AR target proteins[1].
LL-K9-3 (2 μM; 24 h) inhibits MYC- and AR-mediated oncogenic transcriptional programs in 22RV1 cells[1].
LL-K9-3 (0.3-1 μM; 24 h) induces G1-phase cell cycle arrest and significant apoptosis in 22RV1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22RV1
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Concentration:100, 200, 400 nM
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Incubation Time:14 days
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Result:Inhibited colony formation of 22RV1 cells.
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Cell Line:22RV1
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Concentration:0.3 and 1 μM
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Incubation Time:24 h
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Result:Induced cell apoptosis.
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Cell Line:22RV1
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Concentration:0.3 and 1 μM
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Incubation Time:24 h
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Result:Induced G1-phase cell cycle arrest.
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Cell Line:22RV1
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Concentration:0.3 and 1 μM
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Incubation Time:24 h
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Result:Caused a pronounced decrease in phospho-Rpb1 CTD (Ser2) levels, indicating inhibition of CDK9 downstream signaling.
Reduced MCL-1, full-length AR, AR splice variant ARV7, NKX3-1, and KLK3 levels.
化学情報
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CAS 番号 2809353-52-2
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性状 Solid
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分子量 683.95
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分子式 C31H49N5O6S3
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Color White to off-white
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SMILES
O=S(CCNC(CO[C@H]1[C@@H](CC[C@H](C1)C)C(C)C)=O)(N2CCC(CC2)C(NC3=NC=C(SCC4=NC=C(C(C)(C)C)O4)S3)=O)=O
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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
純度とドキュメンテーション
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データシート (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Li J, et al. Discovery of Small-Molecule Degraders of the CDK9-Cyclin T1 Complex for Targeting Transcriptional Addiction in Prostate Cancer. Journal of medicinal chemistry. 2022 Aug 25;65(16):11034-11057. [Content Brief]
[2]. Lin R, et al. Discovery of HyT-Based Degraders of CDK9-Cyclin T1 Complex. Chemistry & biodiversity. 2023 Aug;20(8):e202300769. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
LL-K9-3 関連分類
HY-156084 関連分類
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