SH-17
SH-17 is a STAT3 and HDAC inhibitor, with a Kd of 0.87 μM for STAT3, and IC50 values of 115.2 nM and 9.8 nM for HDAC1 and HDAC6, respectively. SH-17 blocks intracellular ATP production and mitochondrial oxidative phosphorylation, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis. SH-17 is applicable to colon cancer research.
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- Fòrmula: C32H30F3N5O5S
- Peso molecular:653.67
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
STAT3 0.87 μM (Kd) |
HDAC1 115.2 nM (IC50) |
HDAC6 9.8 nM (IC50) |
In Vitro
SH-17 potently inhibits the proliferation of human colon cancer HCT-116 cells with an IC50 of 0.463 μM[1].
SH-17 inhibits proliferation of STAT3-aberrant PANC-1, MDA-MB-468, MDA-MB-231, HepG2, A549, and K562 malignant cells with IC50 values of 2.48-4.85 μM, while showing no cytotoxicity against nonmalignant HUVECs[1].
SH-17 (0.5-2.0 μM; 24 h) concentration-dependently impairs STAT3 phosphorylation at Tyr705 and Ser727, and increases acetylation of HDAC substrates Ac-H3 and Ac-α-tubulin, in human colon cancer HCT-116 cells[1].
SH-17 (Gradient concentrations; 24 h) potently inhibits intracellular ATP production in human colon cancer HCT-116 cells with an IC50 of 0.73 μM[1].
SH-17 (0.33-3.0 μM; 24 h) dose-dependently inhibits mitochondrial OXPHOS, including basal and maximal oxygen consumption rate, and suppresses ATP production in human colon cancer HCT-116 cells[1].
SH-17 (0.0625-0.5 μM; 72 h) induces dose-dependent G0/G1 phase cell cycle arrest and apoptosis in human colon cancer HCT-116 cells, with 26.30% apoptosis observed at 0.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colon cancer HCT-116 cells
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Concentration:0.5, 1.0, 2.0 μM
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Incubation Time:24 h
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Result:Induced a concentration-dependent decrease in phosphorylation of STAT3 at both Tyr705 and Ser727, with dramatic suppression observed at 1.0 μM.
Caused a concentration-dependent increase in acetylation of HDAC substrates Ac-H3 and Ac-α-tubulin, with significant upregulation detected at 2.0 μM.
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Cell Line:human colon cancer HCT-116 cells
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Concentration:0.0625, 0.125, 0.25, 0.5 μM
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Incubation Time:72 h
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Result:Caused dose-dependent apoptosis, with 26.30% of cells apoptotic at 0.5 μM.
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Cell Line:human colon cancer HCT-116 cells
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Concentration:0.0625, 0.125, 0.25, 0.5 μM
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Incubation Time:72 h
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Result:Induced dose-dependent G0/G1 phase cell cycle arrest, with an increase in the proportion of cells in G0/G1 phase and a decrease in S phase cells at all tested concentrations.
Parmacokinetics
| Species | Dose | Route | Cmax | T1/2 | Vz-F_obs | CL | AUC0-24 | F |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 27654 ng/mL | 2.4 h | 0.09 L/kg | 26.3 mL/h/kg | 76323 ng·h/mL | / |
| Rat[1] | 10 mg/kg | s.c. | 3555 ng/mL | 5.8 h | 1.8 L/kg | 216 mL/h/kg | 43580 ng·h/mL | 11.4 % |
| Rat[1] | 10 mg/kg | i.p. | 12110 ng/mL | 4.7 h | 0.55 L/kg | 80.5 mL/h/kg | 121343 ng·h/mL | 31.8 % |
| Rat[1] | 10 mg/kg | p.o. | 391 ng/mL | 3.1 h | 17.1 L/kg | 3491 mL/h/kg | 2947 ng·h/mL | 0.77 % |
Chemical Information
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Peso molecular 653.67
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Fòrmula C32H30F3N5O5S
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SMILES
O=C(C1=CC=C(C(NO)=O)S1)N(CC2)CCC2N(C)C(C=C3C)=CC=C3OC4=CC=C(NC(C5=CC=C(C(F)(F)F)C=C5)=O)C=N4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SH-17 Related Classifications
HY-187212 Related Classifications
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