(±)-trans-BAS-2
(±)-trans-BAS-2 is a hHDAC6 inhibitor with an IC50 value of 0.462 μM. (±)-trans-BAS-2 serves as a scaffold for the design of proteolysis-targeting chimeras (PROTACs) and induces proteasome-dependent degradation of hHDAC6 in cells. (±)-trans-BAS-2 can be used in the research of triple-negative breast cancer and multiple myeloma.
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: 2790482-16-3
- 分子式: C13H21N3O2S
- 分子量:283.39
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
HDAC6 0.462 μM (IC50) |
(±)-trans-BAS-2 (compound 1) (0.462-30 μM; 1 h) potently inhibits recombinant full-length human HDAC6 with an IC50 of 0.462 μM[1].
(±)-trans-BAS-2 (10-12.68 μM; 24 h) induces dose-dependent cell death in MDA-MB-231 triple-negative breast cancer cells with an IC50 of 12.68 μM[1].
(±)-trans-BAS-2 (10-12.68 μM; 24 h) induces dose-dependent cell death in JJN3 multiple myeloma cells with an IC50 of 12.68 μM[1].
(±)-trans-BAS-2 (2 mM; 30 min) does not inhibit recombinant zebrafish HDAC6 CD2 at a concentration of 2 mM[1].
(±)-trans-BAS-2 (50 μM; 24 h) inhibits WT human HDAC6 activity in MDA-MB-231 cells, increasing acetyl-α-tubulin levels, but does not inhibit D567N mutant human HDAC6 activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-231 triple-negative breast cancer cells
-
Concentration:12.68 μM (IC50); 10 μM
-
Incubation Time:24 h
-
Result:Induced dose-dependent cell death in MDA-MB-231 cells, with an IC50 of 12.68 μM for cell death.
Caused 28.72% cell death at 10 μM.
-
Cell Line:JJN3 multiple myeloma cells
-
Concentration:12.68 μM (IC50); 10 μM
-
Incubation Time:24 h
-
Result:Induced dose-dependent cell death in JJN3 cells, with an IC50 of 12.68 μM for cell death.
Caused 28.72% cell death at 10 μM.
-
Cell Line:MDA-MB-231 cells transfected with WT or D567N human HDAC6-FLAG
-
Concentration:50 μM
-
Incubation Time:24 h
-
Result:Significantly increased acetyl-α-tubulin levels in cells transfected with WT human HDAC6-FLAG (densitometry value of ~12 × 104 relative units, normalized to FLAG).
Had no effect on acetyl-α-tubulin levels in cells transfected with D567N human HDAC6-FLAG.
化学情報
-
CAS 番号 2790482-16-3
-
分子量 283.39
-
分子式 C13H21N3O2S
-
SMILES
[H][C@@]12[C@](NC(SCC(N3CCOCC3)=O)=N2)([H])CCCC1
-
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)