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Art. -Nr.: HY-188375

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MB-2-VHL2

MB-2-VHL2 is a Tau PROTAC degrader. MB-2-VHL2 binds to the microtubule-binding region of Tau and recruits the VHL E3 ubiquitin ligase into a ternary complex, mediating Tau ubiquitination and proteasomal degradation. MB-2-VHL2 reduces total Tau and phosphorylated Tau levels in Tau-overexpressing cells and in the hippocampus of wild-type mice, and improves recognition memory and spatial learning ability in mouse models, while reducing hippocampal phosphorylated Tau and oligomeric Tau levels and altering Tau aggregation patterns. MB-2-VHL2 can be used for research on Alzheimer's disease.
(Pink: Tau Protein ligand (HY-188376); Blue: VHL ligand (HY-173435); Black: linker (HY-W004945)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3114837-73-6
Formel: C₄₈H₆₃N₉O₈S₂
Molecular Weight:958.20

Speicherung:

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

Data Sheet (285 KB)

MB-2-VHL2 Chemical Structure

CAS. Nr.: 3114837-73-6

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Preis

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MB-2-VHL2 is a Tau PROTAC degrader. MB-2-VHL2 binds to the microtubule-binding region of Tau and recruits the VHL E3 ubiquitin ligase into a ternary complex, mediating Tau ubiquitination and proteasomal degradation. MB-2-VHL2 reduces total Tau and phosphorylated Tau levels in Tau-overexpressing cells and in the hippocampus of wild-type mice, and improves recognition memory and spatial learning ability in mouse models, while reducing hippocampal phosphorylated Tau and oligomeric Tau levels and altering Tau aggregation patterns. MB-2-VHL2 can be used for research on Alzheimer's disease^[1]. (Pink: Tau Protein ligand (HY-188376); Blue: VHL ligand (HY-173435); Black: linker (HY-W004945)).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

Aβ/Tau/α-Synuclein AggregationProtein/Amino Acid MetabolismOthers

Aβ/Tau/α-Synuclein Aggregation

MB-2-VHL2 (24 h) reduces eGFP-Tau fluorescence in HEK293T-eGFP-Tau cells^[1].
MB-2-VHL2 (2-200 μM) reduces total Tau and pS396-Tau in HEK293T-eGFP-Tau lysates^[1].

Aβ/Tau/α-Synuclein Aggregation

Protein/Amino Acid Metabolism

MB-2-VHL2 reduces Tau in HEK293T-eGFP-Tau cells through the ubiquitin-proteasome system, because MG132 (HY-13259) restores Tau and increases ubiquitin signals; moreover, excess free VHL ligand partially attenuates MB-2-VHL2-mediated Tau degradation, supporting VHL-dependent degradation^[1].

Others

MB-2-VHL2 (1-500 μM; 24 h) does not reduce cell viability in HEK293T cells even at concentrations up to 500 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:

HEK293T cells
Concentration:

1, 10, 50, 200, and 500 μM
Incubation Time:

24 h
Result:

Did not reduce viability at concentrations up to 500 μM.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_last	T_max (Brain)	C_max (Brain)
Mice^[1]	3 mg/kg	s.c.	2 h	1101.4 ng/mL	4131.7 ng·h/mL	10 min	55.4 ng/g

In Vivo

Aβ/Tau/α-Synuclein Aggregation

MB-2-VHL2 (2.5 μL, 800 μM; i.c.v.; single injection) reduces hippocampal total Tau and pS396-Tau after a single ICV administration in wild-type mice^[1].
MB-2-VHL2 (3 mg/kg; s.c.) reduces total Tau and p-Tau in the hippocampus of wild-type mice at 24 hours after administration or on days 2 and 4 after administration^[1].
MB-2-VHL2 (3 mg/kg; s.c.; once every 7 days; 28 days) improves recognition memory and spatial learning ability in 3 x Tg-AD mice and reduces hippocampal p-Tau^[1].

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

Animal Model:

C57BL/6J (male, 6 months old for the ICV cohort)^[1]
Dosage:

2.5 μL of 800 μM
Administration:

i.c.v.; single injection
Result:

Reduced hippocampal total Tau and pS396-Tau after a single ICV dose in wild-type mice.

Animal Model:

3xTg-AD (male; 57BL/6JGpt-Tg(Thy-APP/Thy-PSEN1/Thy-MAPT)17/Gpt)^[1]
Dosage:

3 mg/kg
Administration:

s.c.; every 7 days; 28 days
Result:

Improved recognition memory and spatial learning and reduces hippocampal p-Tau in 3 x Tg-AD mice.

Related Protocols :

Chemical Information

CAS. Nr. 3114837-73-6
Molecular Weight 958.20
Formel C₄₈H₆₃N₉O₈S₂
SMILES

O=C(N1C2=C(C=C(N(C)C)C=C2)SC3=CC(N(C)C)=CC=C13)NCCNC(COCCOCC(N[C@@H](C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)C(C)(C)C)=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 (285 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]. Zhao T, et al. Tau-Targeted PROTACs Degrade Pathology-Associated Tau and Improve Memory in Alzheimer's Disease Models. ACS Chem. Biol., 2026, 21(8): 1906-1916.

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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MB-2-VHL2

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

MB-2-VHL2 Related Classifications

HY-188375 Related Classifications

Bioz

Keywords

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