2. Apoptosis
  3. MDM-2/p53 Apoptosis
  4. 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].

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (ADH-6 TFA) usually boasts enhanced water solubility and stability.

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

ADH-6 Chemical Structure

ADH-6 Chemical Structure

CAS No. : 2227429-65-2

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ADH-6 Related Antibodies

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Description

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].

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.

ADH-6 Related Antibodies

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: Cmax: 21 µg/mL, T1/2: 3.6 h
Molecular Weight

640.64

Formula

C29H36N8O9
CAS No.
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
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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ADH-6 Related Classifications

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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.

Keywords:

ADH-62227429-65-2ADH6ADH 6MDM-2/p53Apoptosistripyridylamideself-assemblyp53transcriptionalcell cycleapoptosiscancerInhibitorinhibitorinhibit

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