J594
J594 is a BRD4 molecular glue degrader targeting RNF126, with DC50 values of 0.077 μM (long-form BRD4 in HEK293T cells) and 0.26 μM (short-form BRD4 in HEK293T cells), respectively. J594 induces proteasome- and RNF126-dependent degradation of BRD4.
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。
- CAS 番号: 3036531-21-9
- 分子式: C34H32Cl2N6O4S
- 分子量:691.63
-
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
BRD4 |
RNF126 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | DC50 |
0.077 μM
|
Degradation of long BRD4 isoform in human HEK293T cells assessed by Western blotting after 16 h of treatment.
Degradation of long BRD4 isoform in human HEK293T cells assessed by Western blotting after 16 h of treatment.
|
41867716 |
| HEK-293T | DC50 |
0.26 μM
|
Degradation of short BRD4 isoform in human HEK293T cells assessed by Western blotting after 16 h of treatment.
Degradation of short BRD4 isoform in human HEK293T cells assessed by Western blotting after 16 h of treatment.
|
41867716 |
体外実験
J594 (0.0001-50 μM; 30 min) covalently binds to purified RNF126 protein in a dose-dependent manner, as demonstrated by competition assays with IA-rhodamine labeling[1].
J594 (0.01-10 μM; 16 h) potently and selectively degrades both long and short isoforms of BRD4 in a proteasome-dependent manner in HEK293T cells, with DC50 values of 0.077 μM and 0.26 μM, respectively[1].
J594 (0.1-1 μM; 10 h)-mediated BRD4 degradation depends on RNF126, as the degradation of both long and short BRD4 isoforms in HEK293T cells is significantly inhibited in RNF126-knockout cells compared with wild-type cells[1].
J594 (1 μM; 24 h) exhibits high target selectivity in MDA-MB-231 cells, where BRD4 is the major protein significantly downregulated[1].
J594 (0.1-10 μM; 24 h) exhibits only extremely low cytotoxicity in HEK293T, OVISE and MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
Cell Line:HEK293T cells
-
Concentration:0.01, 0.1, 0.5, 1, 2.5, 5, 10 μM
-
Incubation Time:16 h
-
Result:Induced dose-dependent degradation of both long and short BRD4 isoforms, with no appreciable loss of BRD2 or BRD3.
Achieved DC50 of 0.077 μM for long BRD4 and 0.26 μM for short BRD4.
-
Cell Line:RNF126 wild-type and knockout HEK293T cells
-
Concentration:0.1, 1 μM
-
Incubation Time:10 h
-
Result:Induced significant degradation of both long and short BRD4 isoforms in RNF126 wild-type HEK293T cells.
Showed significantly attenuated BRD4 degradation in RNF126 knockout HEK293T cells.
-
Cell Line:HEK293T, OVISE ovarian cancer, and MDA-MB-231 breast cancer cells
-
Concentration:0.1, 1, 10 μM
-
Incubation Time:24 h
-
Result:Showed minimal effects on cell viability across the tested concentration range in all three cell lines.
化学情報
-
CAS 番号 3036531-21-9
-
分子量 691.63
-
分子式 C34H32Cl2N6O4S
-
SMILES
CC1=NN=C2N1C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(N[C@H]5C[C@H](NC(/C=C/C(C6=C(Cl)C=C(OC)C=C6)=O)=O)C5)=O
-
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)
J594 関連分類
HY-187457 関連分類
Powered by Bioz