YDH-704
YDH-704 is a PAK1/HDAC10 inhibitor, with IC50 values of 0.05 μM and 0.02 μM against human targets, respectively. YDH-704 blocks PAK1-mediated oncogenic signaling pathways, inhibits the proliferation and migration of tumor cells, suppresses the epigenetic regulatory function of HDAC10, downregulates PD-L1 expression, and regulates polyamine metabolism. YDH-704 reduces MDSC/Treg infiltration, enhances the infiltration and activation of CD8+ T cells, and inhibits tumor growth and lung metastasis. YDH-704 can be used for research on triple-negative breast cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C31H35ClN8O4
- Peso molecular:619.11
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Almacenamiento:
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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Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC10 0.02 μM (IC50) |
PAK1 0.05 μM (IC50) |
In Vitro
YDH-704 (compound 28a) potently and selectively inhibits purified PAK1 (IC50 = 0.05 μM) and HDAC10 (IC50 = 0.02 μM), and exhibits extremely low activity against other HDAC subtypes and most human kinases[1].
YDH-704 (8 μM; 6 h) directly binds to and stabilizes PAK1 and HDAC10 proteins in triple-negative breast cancer (TNBC) cells, confirming target binding at the cellular level[1].
YDH-704 (2-8 μM; 24 h) dose-dependently inhibits the activation of PAK1 and HDAC10, reduces phosphorylated PAK1 levels, and increases acetylated H3K27 levels in BT-549 and MDA-MB-231 triple-negative breast cancer (TNBC) cells[1].
YDH-704 (1 μM; 24 h) significantly increases the level of N8-AcSpd in MDA-MB-231 cells, confirming that it inhibits the polyamine deacetylase activity of HDAC10 in cells[1].
YDH-704 (24-48 h) potently inhibits the proliferation of BT-549 and MDA-MB-231 triple-negative breast cancer (TNBC) cells, with IC50 values ranging from 0.44 to 1.25 μM[1].
YDH-704 (2-8 μM; 24 h) inhibits the proliferation and long-term colony formation of triple-negative breast cancer (TNBC) cells in a dose-dependent manner; it downregulates PD-L1 expression in BT-549 and 4T1 cells in a dose-dependent manner via an HDAC10-dependent mechanism[1].
YDH-704 (2-8 μM; 24-48 h) inhibits the in vitro migration of triple-negative breast cancer (TNBC) cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TNBC cells
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Concentration:2, 4, 8 μM
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Incubation Time:24 h
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Result:Dose-dependently reduced the proportion of EdU-positive cells, indicating reduced proliferation, with superior efficacy compared to FRAX486, DKFZ-748, or their combination.
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Cell Line:TNBC cells
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Concentration:2, 4, 8 μM
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Incubation Time:24 h (Transwell)
24, 48 h (wound healing) -
Result:Dose-dependently reduced TNBC cell migration in both Transwell and wound healing assays, with superior efficacy compared to FRAX486, DKFZ-748, or their combination.
Parmacokinetics
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2 | Tmax | CLz/F | Vz/F | Cmax |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 7065.77 μg/L·h | 7073.05 μg/L·h | 3.14 h | 3.18 h | 2.36 h | 0.42 h | 1.47 L/h/kg | 5.13 L/kg | 2416.06 μg/L |
In Vivo
YDH-704 (5-10 mg/kg; i.p.; 1-11 days) dose-dependently inhibits the growth of BT-549 triple-negative breast cancer (TNBC) xenografts in mice, with better efficacy than single-target inhibitors and their combination therapies; it also dose-dependently suppresses lung metastasis of triple-negative breast cancer in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 619.11
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Fòrmula C31H35ClN8O4
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SMILES
ClC1=C(C=CC(C2=NC(C)=CC=C2)=C1)C3=CC4=C(N(C3=O)CC(NCCN(C)CCCC(NO)=O)=O)N=C(NC5CC5)N=C4
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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)
YDH-704 Related Classifications
HY-187370 Related Classifications
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