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Art. -Nr.: HY-145818

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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)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2669785-84-4
Formel: C₄₉H₆₅N₇O₇S
Molecular Weight:896.15

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

JPS035 Chemical Structure

CAS. Nr.: 2669785-84-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
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Biologische Aktivität

Beschreibung

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^[1]. (Pink: HDAC1 and HDAC2 and HDAC3 ligand (HY-50934); Blue: VHL ligand (HY-136164); Black: linker (HY-W105741)).

IC₅₀ & Target

^[1]

HDAC1

3.58 μM (DC₅₀)

HDAC2

VHL

HDAC3

1.38 μM (DC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

HCT116 human colon carcinoma cells
Concentration:

0.1 μM, 1 μM, 10 μM
Incubation Time:

24 h
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

CAS. Nr. 2669785-84-4
Molecular Weight 896.15
Formel C₄₉H₆₅N₇O₇S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Smalley JP, et al. Optimization of Class I Histone Deacetylase PROTACs Reveals that HDAC1/2 Degradation is Critical to Induce Apoptosis and Cell Arrest in Cancer Cells. J Med Chem. 2022;65(7):5642-5659. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
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- IC₅₀ & Target
- In Vitro
Chemical Information
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JPS035

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

In Vitro

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

JPS035 Related Classifications

HY-145818 Related Classifications

Bioz

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