MS479
MS479 is a PROTAC degrader targeting BRD4, BRD3 and BRD2. MS479 recruits the E3 ligase SPOP by bridging the protein GLP, thereby promoting polyubiquitination modification and subsequent 26S proteasomal degradation. MS479 inhibits the proliferation of colorectal cancer cells and can be used for research on colorectal cancer and triple-negative breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: SPOP ligand (HY-176036); Black: linker (HY-176037)).
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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。
- 分子式: C59H82ClN11O5S
- 分子量:1092.87
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
PROTACs 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
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | DC50 |
6.2 μM
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Degradation of BRD4 short isoform (BRD4 (S)) in human HT29 colorectal cancer cells assessed via Western blot-based protein degradation assay incubated for 24 hrs.
Degradation of BRD4 short isoform (BRD4 (S)) in human HT29 colorectal cancer cells assessed via Western blot-based protein degradation assay incubated for 24 hrs.
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40202531 |
| HT-29 | GI50 |
4.5 μM
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Antiproliferative activity against human HT29 colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay.
Antiproliferative activity against human HT29 colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay.
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40202531 |
体外実験
MS479 binds with high affinity to purified recombinant BRD4-BD2 (KD=200 nM) and GLP-SET domain (KD=306 nM)[1].
MS479 (0.156-10 μM; 2-72 h) induces concentration- and time-dependent degradation of BRD4 (S), weak degradation of BRD4 (L), BRD3, and BRD2, and potent suppression of c-MYC in HT29 cells, with BRD4 (S) degradation dependent on BRD4, GLP, and the ubiquitin-proteasome system[1].
MS479 (1-10 μM; 24 h) regulates BRD4, BRD3, and BRD2 protein levels via a post-translational mechanism and downregulates c-MYC transcription in HT29 cells[1].
MS479 (0.1-5 μM; 24 h) degrades BRD4 (S), BRD3, BRD2, and BRD4 (L) in MDA-MB-231 cells, with greater activity against BRD4 (L) than in HT29 cells[1].
MS479 (0.021-10 μM; 72 h) potently inhibits proliferation of HT29 colorectal cancer cells (GI50=4.5 μM) without affecting viability of normal PNT2 prostatic epithelial cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT29 colorectal cancer cells
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Concentration:0.156-10 μM (24 h); 5 μM (2 h, 4 h, 8 h, 16 h, 48 h, 72 h); 1 μM (pretreatment with MS1262, JQ1, MLN4924)
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Incubation Time:2 h (pretreatment); 2 h, 4 h, 8 h, 16 h, 24 h, 48 h, 72 h (MS479 treatment)
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Result:Induced >50% degradation of BRD4 short isoform (BRD4 (S)) at 5 μM for 24 h.
Induced degradation of BRD4 (S) with a DC50 of 6.2 μM and maximum degradation (D_max) of 63% in concentration-dependent testing.
Induced ~50% degradation of BRD4 long isoform (BRD4 (L)), weak degradation of BRD3 and BRD2, and complete suppression of c-MYC at 10 μM for 24 h.
Induced BRD4 (S) degradation detectable at 16 h and persisting to 72 h in time-dependent testing.
Required 48 h or longer for effective degradation of BRD4 (L), BRD3, and BRD2 in time-dependent testing.
Caused c-MYC levels to drop sharply starting at 2 h in time-dependent testing.
Degradation of BRD4 (S) was rescued by pretreatment with MS1262, JQ1, or MLN4924.
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Cell Line:HT29 colorectal cancer cells
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Concentration:1-10 μM
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Incubation Time:24 h
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Result:Did not alter mRNA levels of BRD4 (S), BRD4 (L), BRD3, or BRD2.
Significantly downregulated c-MYC mRNA at 5 μM and 10 μM.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:0.1-5 μM
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Incubation Time:24 h
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Result:Induced degradation of BRD4 (S), BRD3, and BRD2.
Showed enhanced activity against BRD4 (L) compared to HT29 cells.
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Cell Line:HT29 colorectal cancer cells, PNT2 normal prostatic epithelial cells
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Concentration:0.021-10 μM
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Incubation Time:72 h
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Result:Inhibited HT29 cell proliferation with a GI50 of 4.5 μM.
Did not suppress proliferation of PNT2 cells at any tested concentration.
化学情報
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分子量 1092.87
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分子式 C59H82ClN11O5S
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SMILES
CC1=NN=C2[C@@H](N=C(C3=C(N21)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCCCCCCCCCNC(CCCN5CCC(NC6=C7C=C(OC)C(OCCCN8CCCC8)=CC7=NC(N9CCOCC9)=C6)CC5)=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
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)
MS479 関連分類
HY-176035 関連分類
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