1. PROTAC Metabolic Enzyme/Protease
  2. PROTACs 11β-HSD
  3. PROTAC 11β-HSD1 Degrader 1

PROTAC 11β-HSD1 Degrader 1 is a highly efficient PROTAC targeting 11β-HSD1 (Hydroxysteroid 11-beta dehydrogenase 1). PROTAC 11β-HSD1 Degrader 1 demonstrates ubiquitin-proteasome-dependent degradation of 11β-HSD1. PROTAC 11β-HSD1 Degrader 1 can be used for the study of type 2 diabetes mellitus (T2DM).
(Pink: 11β-HSD1 Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker (HY-42490)).

For research use only. We do not sell to patients.

PROTAC 11β-HSD1 Degrader 1

PROTAC 11β-HSD1 Degrader 1 Chemical Structure

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Description

PROTAC 11β-HSD1 Degrader 1 is a highly efficient PROTAC targeting 11β-HSD1 (Hydroxysteroid 11-beta dehydrogenase 1). PROTAC 11β-HSD1 Degrader 1 demonstrates ubiquitin-proteasome-dependent degradation of 11β-HSD1. PROTAC 11β-HSD1 Degrader 1 can be used for the study of type 2 diabetes mellitus (T2DM)[1]. (Pink: 11β-HSD1 Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker (HY-42490)).

In Vitro

PROTAC 11β-HSD1 Degrader 1 (Compound 25) (0.12-10 μM, 48 h) can effectively degrade 11β-HSD1 in the MV-4-11 cell line[1].

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

Western Blot Analysis[1]

Cell Line: MV-4-11 cell
Concentration: 0.12 μM, 0.37 μM, 1.1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Dose-dependent degradation of 11β-HSD1 in the MV-4-11 cell line.
In Vivo

PROTAC 11β-HSD1 Degrader 1 (Compound 25) (50 mg/kg, i.p., once every two days for 2 weeks) can effectively improve glucose homeostasis in mice with type 2 diabetes induced by a high-fat diet[1].

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

Animal Model: 6-week-old male C57BL/6J wild-type mice were fed a high-fat diet for eight weeks[1].
Dosage: 50 mg/kg
Administration: I.p., once every two days for 2 weeks
Result: Significantly improved glucose tolerance in mice.
Enhanced glucose-stimulated insulin secretion.
Showed a decreasing trend in body weight and random blood glucose levels.
Molecular Weight

1118.39

Formula

C59H79N11O9S

SMILES

O=C(C1=C(C(C)(C)C)N(C2=CC=C(C(NCC3=CN(CCOCCOCCOCCC(N[C@H](C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)C(C)(C)C)=O)N=N3)=O)C=C2)N=C1)NC78CC9CC(C8)CC(C9)C7

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PROTAC 11β-HSD1 Degrader 1
Cat. No.:
HY-179602
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