Colletofragarone A2

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Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo.

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Colletofragarone A2 Chemical Structure

CAS No. : 181377-06-0

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

HSP90

In Vitro

Mutant p53 loses original tumor suppressor function but acquires new abilities regarding oncogenic progression^[1].
Colletofragarone A2 (0.05-5 μM; 72 h) shows high selectivity and more cytotoxic activity on cells with p53^R175H structural mutants than with other p53 statuses such as a DNA-contact mutant, wild-type, and null cells^[1].
Colletofragarone A2 (2 μM; 8 h) decreases mutant p53 levels in SK-BR-3 (p53^R175H) cells by promoting p53 degradation^[1].
Colletofragarone A2, combinded with 10 μM MG-132 (HY-13259), (2 or 4 μM; 4 h) induces the accumulation of the aggregated mutant p53^[1].

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

Western Blot Analysis^[1]

Cell Line:	SK-BR-3 (p53^R175H), HuCCT1 (p53^R175H), Saos-2 (p53^R175H), OVCAR-3 (p53^R248Q), and A549 (wild-type p53)
Concentration:	0, 0.5, 1, 2, 4 μM
Incubation Time:	4 hours
Result:	Decreased the mutant p53^R175H levels in SK-BR-3 and HuCCT1 cells in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	SK-BR-3 (p53^R175H) cells
Concentration:	2 μM, 4 μM (with 10 μM MG-132 (HY-13259), respectively)
Incubation Time:	4 hours
Result:	Promoted the proteasome-mediated degradation of mutant p53 and the accumulation of precipitated mutant p53.

Cell Viability Assay^[1]

Cell Line:	SK-BR-3 (p53^R175H), HuCCT1 (p53^R175H), OVCAR-3 (p53^R248Q), and A549 (wild-type p53) cells
Concentration:	0.05-5 μM
Incubation Time:	72 hours
Result:	Decreased the level of p53 and showed high selectivity and more cytotoxic activity on cells with p53^R175H structural mutants, IC50s of 0.18 μM (SK-BR-3), 0.35 μM (HuCCT1), respectively.

In Vivo

Colletofragarone A2 (0.35 mM, 100 μL; injected intratumorally and daily; 13 d) markedly decreases tumor cell growth in mouse infected with HuCCT1 (p53^R175H) cells^[1].

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

Animal Model:	Xenograft model with HuCCT1 (p53^R175H) cells in mouse^[1]
Dosage:	0.35 mM with 100 μL (DMSO solution)
Administration:	Injected intratumorally; daily; 13 days; tested tumor growth at 1, 3, 5, 7, 9, 13 days
Result:	Inhibited tumor growth without lowing body weight of mouse.

Molecular Weight

386.44

Formula

C₂₂H₂₆O₆

CAS No.

181377-06-0

SMILES

C/C=C/C=C/C=C/C1=C2[C@@]3([H])[C@@](C=CC([C@@]3([H])[C@H](O)C[C@H](O)C[C@H](C)OC2=O)=O)([H])O1

Structure Classification

Initial Source

Microorganisms

Colletotrichum sp.

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Sadahiro Y, et al. Colletofragarone A2 Inhibits Cancer Cell Growth In Vivo and Leads to the Degradation and Aggregation of Mutant p53. Chem Res Toxicol. 2022 Aug 26. [Content Brief]