JPS035
JPS035 is a HDAC1, HDAC2 and HDAC3 PROTAC degrader, with a DC50 value of 3.58 μM against HDAC1 and 1.38 μM against HDAC3. JPS035 recruits the VHL E3 ligase to mediate the ubiquitination and degradation of HDAC1, HDAC2 and HDAC3. JPS035 increases the acetylation level of histone H3 lysine 56 and regulates global gene expression. JPS035 can be used in colon cancer-related research.
(Pink: HDAC1 and HDAC2 and HDAC3 ligand (HY-50934); Blue: VHL ligand (HY-136164); Black: linker (HY-W105741)).
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- No. CAS: 2669785-84-4
- Fòrmula: C49H65N7O7S
- Peso molecular:896.15
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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HDAC1 3.58 μM (DC50) |
HDAC2 |
VHL |
HDAC3 1.38 μM (DC50) |
JPS035 (0.1-10 μM; 24 h) induces degradation of HDAC1, HDAC2, and HDAC3 in HCT116 cells with DC50 values of 3.58 μM (HDAC1) and 1.38 μM (HDAC3), and maximal degradation levels of 68%, 49%, and 76% for HDAC1, HDAC2, and HDAC3, respectively[1].
JPS035 (10 μM; 24 h) induces limited transcriptome changes in HCT116 cells, with 243 upregulated and 27 downregulated significant differentially expressed genes after 24 h of 10 μM treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 human colon carcinoma cells
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Concentration:0.1 μM, 1 μM, 10 μM
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Incubation Time:24 h
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Result:Induced HDAC1 and HDAC2 degradation comparable to reference PROTAC 1 (JPS004) at 10 μM.
Promoted HDAC3 degradation without exhibiting a hook effect at 10 μM.
Achieved maximal degradation (Dmax) values of 68% for HDAC1, 49% for HDAC2, and 76% for HDAC3.
Reached half-maximal degradation concentration (DC50) of 3.58 μM for HDAC1 and 1.38 μM for HDAC3; no DC50 was determined for HDAC2.
Chemical Information
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No. CAS 2669785-84-4
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Peso molecular 896.15
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Fòrmula C49H65N7O7S
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SMILES
CC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)O)C(NCC2=C(C=C(C3=C(C)N=CS3)C=C2)OCCCCCCCCCCCC(NC4=CC=C(C=C4)C(NC5=C(C=CC=C5)N)=O)=O)=O)=O)=O
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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)
JPS035 Related Classifications
HY-145818 Related Classifications
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