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Cat. No.: 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)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 2669785-84-4
화학식: C₄₉H₆₅N₇O₇S
분자량:896.15

보관:

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

Data Sheet (270 KB)

JPS035 Chemical Structure

CAS No.: 2669785-84-4

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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)

All HDAC Isoforms :

All PROTACs Isoforms :

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 No. 2669785-84-4
분자량 896.15
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 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)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

견적 받기

Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

JPS035

All HDAC Isoforms

All PROTACs Isoforms

Biological Activity

제품 설명

IC50 & Target

In Vitro

Chemical Information

순도&문서

References

Calculators

Help & FAQs

JPS035 Related Classifications

HY-145818 Related Classifications

Bioz

Keywords

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