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Cat. No.: HY-174858

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dASK1-VHL

dASK1-VHL is an ASK1 PROTAC degrader that recruits VHL. dASK1-VHL induces ubiquitination and proteasomal degradation of ASK1 by forming a ternary complex, and inhibits the downstream p38 MAPK signaling pathway. dASK1-VHL can be used in studies of metabolic dysfunction-associated steatohepatitis.
(Pink: ASK1 ligand (HY-174860); Blue: VHL ligand (HY-125845); Black: linker).

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Formule: C₄₈H₅₇F₂N₁₁O₈S
Masse moléculaire:986.10

Stockage:

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

Data Sheet (277 KB)

dASK1-VHL Chemical Structure

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Use of MCE Products

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

Activité biologique
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

dASK1-VHL is an ASK1 PROTAC degrader that recruits VHL. dASK1-VHL induces ubiquitination and proteasomal degradation of ASK1 by forming a ternary complex, and inhibits the downstream p38 MAPK signaling pathway. dASK1-VHL can be used in studies of metabolic dysfunction-associated steatohepatitis^[1]. (Pink: ASK1 ligand (HY-174860); Blue: VHL ligand (HY-125845); Black: linker).

Voir tous les produits spécifiques à Isoform PROTACs :

Voir tous les produits spécifiques à Isoform p38 MAPK :

In Vitro

dASK1-VHL (compound 60) (1 nM-10 μM; 8 h) is a potent VHL-dependent PROTAC that induces dose-dependent degradation of ASK1 in HepG2 cells^[1].
dASK1-VHL (1 nM-10 μM) shows no cytotoxicity in the tested cell lines over the concentration range of 1 nM to 10000 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HepG2 cells
Concentration:

1, 10, 100, 500, 1000, 10000 nM
Incubation Time:

8 h
Result:

Dose-dependently degraded ASK1, achieving maximum degradation (~60% reduction) at 50 nM.
Showed reduced efficacy at concentrations ≥ 100 nM, consistent with the Hook effect.
Had its ASK1 degradation completely abrogated by pretreatment with VH032, confirming VHL-dependent action.
Exhibited no detectable cytotoxicity across a wide concentration range (1 nM to 10 μM).

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-inf	CL_plasma	V_ss	C_max	T_max	F
Mice^[1]	20 mg/kg	p.o.	/	12913.87 ng·h/mL	/	/	9429.3 ng/mL	1.00 h	47.48 %
Mice^[1]	2 mg/kg	i.v.	0.55 h	2719.67 ng·h/mL	11.36 mL/min/kg	0.40 L/kg	/	/	/

In Vivo

dASK1-VHL (compound 60) (2 mg/kg; i.p.; once daily; for 14 consecutive days) effectively degrades hepatic ASK1 via a post-translational mechanism, inhibits the ASK1-p38 MAPK signaling pathway, and alleviates hepatic lipid accumulation in a mouse MASH model induced by an MCD diet^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 (male, 6-8 weeks old, MCD diet-induced MASH)^[1]
Dosage:

2 mg/kg
Administration:

i.p.; once daily; 14 days
Result:

Reduced hepatic ASK1 protein levels.
Decreased phosphorylation of p38 MAPK.
Reduced ASK1 ubiquitination in liver tissue.
Decreased hepatic lipid accumulation.
Left ASK1 mRNA expression unchanged relative to controls.
Did not alter protein levels of TAK1.

Chemical Information

Masse moléculaire 986.10
Formule C₄₈H₅₇F₂N₁₁O₈S
SMILES

O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(NC(CCC(NCCOCCC(N[C@H](C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)=O)C(C)(C)C)=O)=O)=O)=C(F)C=C3F
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 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)
Instruction de manipulation (2659 KB)

Références

[1]. Sarkar HS, et al. Rational design and discovery of potent PROTAC degraders of ASK1: a targeted therapy in MASH. RSC medicinal chemistry. 2025 Aug 13;16(8):3469-3494. [Content Brief]

Calculators

Calculateur de molarité

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

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Calculateur de dilution

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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

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100 mg

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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dASK1-VHL

Voir tous les produits spécifiques à Isoform PROTACs

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