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Art. -Nr.: HY-145785

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ADH-6

ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases[1].

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CAS. Nr.: 2227429-65-2
Formel: C₂₉H₃₆N₈O₉
Molecular Weight:640.64

Speicherung:

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

Data Sheet (275 KB)

ADH-6 Chemical Structure

CAS. Nr.: 2227429-65-2

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

In Vitro

ADH-6 (25 μM, 10 h) inhibits aggregation of pR248W (indicated by dot blot assay)^[1].
ADH-6 (5 μM, 6 h) dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells^[1].
ADH-6 (0-10 μM, 24 or 48 h) causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2)^[1].
ADH-6 (5 μM, 24 h) specifically targets and reactivates aggregation-prone mutant p53 in MIA PaCa-2 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

MIA PaCa-2 (mutant R248W p53), SK-BR-3 (mutant R175H p53)
Concentration:

0, 2.5, 5, 7.5, 10 μM
Incubation Time:

24, 48 h
Result:

Caused death of cancer cells bearing mutant, but not WT, p53.

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2 cells
Concentration:

5 μM
Incubation Time:

24 h
Result:

Increased expression of p53-inducible MDM2 and proapoptotic Bax.

In Vivo

ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) causes regression of mutant p53-bearing tumors ^[1].

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

Animal Model:

MIA PaCa-2 xenografts^[1]
Dosage:

716.4 µM in 0.02% DMSO
Administration:

Intraperitoneal injection, every 2 days, for a total of 12 doses
Result:

Reduced tumor growth relative to the saline-treated control group.
Reduced mutant p53 levels and shrinked xenografts harboring aggregation-prone mutant p53.

Animal Model:

MIA PaCa-2 xenografts (pharmacokinetics assay)^[1]
Dosage:

15 mg/kg
Administration:

Intraperitoneal injection, for a single dose
Result:

C_max: 21 µg/mL, T_1/2: 3.6 h

Chemical Information

CAS. Nr. 2227429-65-2
Molecular Weight 640.64
Formel C₂₉H₃₆N₈O₉
SMILES

O=C(C1=NC(OCCCN)=C(NC(C2=NC(OCCCN)=C(NC(C3=NC(OCCCC)=C([N+]([O-])=O)C=C3)=O)C=C2)=O)C=C1)OC
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 (275 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]. Palanikumar L, et al. Protein mimetic amyloid inhibitor potently abrogates cancer-associated mutant p53 aggregation and restores tumor suppressor function. Nat Commun. 2021;12(1):3962. [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.

Keywords

100 mg

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