Hsp90-IN-15

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Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell.

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Hsp90-IN-15 Chemical Structure

CAS No. : 2252283-32-0

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Description

Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell^[1].

IC₅₀ & Target

HSP90

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	19.6 μM Compound: 22g	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31928863]
HepG2	IC₅₀	16.1 μM Compound: 22g	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31928863]
MDA-MB-231	IC₅₀	22.1 μM Compound: 22g	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31928863]

In Vitro

Hsp90-IN-15 (compound 22g) againsts HeLa, HepG2, and MDA-MB-23 cells with IC50s of 19.6 μM, 16.1 μM, and 22.1 μM, respectively^[1].
Hsp90-IN-15 binds with Hsp90^N, and the △Tm value is 10.92 °C^[1].
Hsp90-IN-15 (0-20 μM; 48 h) arrests cell cycle at S phase in a dose-dependent manner^[1].
Hsp90-IN-15 (0-20 μM; 48 h) exhibits an accumulation of early and late apoptotic cells in a time and dose dependent manner^[1].
Caspase-3 is an executioner caspase and modifies apoptosis proteins^[1].
Hsp90-IN-15 (0-50 μM; 48 h) increases the expression of Bax and cleaved-caspase 3, as well as downregulates the levels of Bcl-2, pro-caspase 3 and Hsp90^[1].

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

Cell Viability Assay^[1]

Cell Line:	HeLa cells
Concentration:	0, 5, 10, 20 μM
Incubation Time:	48 hours
Result:	Arrested cell cycle at S phase dose-dependently.

Apoptosis Analysis^[1]

Cell Line:	HeLa cells
Concentration:	0, 5, 10, 20 μM
Incubation Time:	48 hours
Result:	Induced apoptosis in HeLa cells.

Western Blot Analysis^[1]

Cell Line:	HeLa cells
Concentration:	0, 12.5, 25, 50 μM
Incubation Time:	48 hours
Result:	Decreased the level of Hsp90 and increased the proportion of Bax/Bcl-2 as well.

Molecular Weight

416.48

Formula

C₂₃H₂₇F₃N₄

CAS No.

2252283-32-0

SMILES

[H][C@@]12CCCN3CCC[C@@]([C@@]31[H])([C@]4(CCC5=C(C6=C(N=C5N4C2)C=CC(C(F)(F)F)=C6)N)[H])[H]

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]. Xu Y, et al. New modification strategy of matrine as Hsp90 inhibitors based on its specific L conformation for cancer treatment. Bioorg Med Chem. 2020 Feb 15. 28(4):115305. [Content Brief]

Hsp90-IN-15 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:

Hsp90-IN-152252283-32-0HSPHeat shock proteinsL-shaped matrine derivativesanticancer activitytargeted modificationMDA-MB-231HepG2HeLaInhibitorinhibitorinhibit

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