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Art. -Nr.: HY-189694

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SH458

SH458 is an orally active anti-triple-negative breast cancer compound. SH458 significantly upregulates the expression of unfolded protein response (UPR)-related proteins, including p-eIF2α and p-IRE1α. SH458 induces Apoptosis, G2/M phase arrest, oxidative stress with increased ROS, DNA damage, and checkpoint kinase activation.

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CAS. Nr.: 3109470-77-8
Formel: C₂₈H₃₀N₂O₄
Molecular Weight:458.55

Speicherung:

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

SH458 Chemical Structure

CAS. Nr.: 3109470-77-8

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

eIF2-α

IRE1α

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Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	0.23 μM	Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay. Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay.	42748754
MDA-MB-468	IC50	0.14 μM	Antiproliferative activity against human MDA-MB-468 cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay. Antiproliferative activity against human MDA-MB-468 cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay.	42748754
SUM149PT	IC50	0.25 μM	Antiproliferative activity against human SUM149T/SUM149PT cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay. Antiproliferative activity against human SUM149T/SUM149PT cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay.	42748754
4T1	IC50	0.28 μM	Antiproliferative activity against murine 4T1 cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay. Antiproliferative activity against murine 4T1 cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay.	42748754
MCF-10A	IC50	50 μM	Antiproliferative activity against normal human mammary epithelial MCF10A cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay with IC50 greater than 50 μM. Antiproliferative activity against normal human mammary epithelial MCF10A cells assessed as viability reduction after 72 hrs incubation by sulforhodamine B (SRB) assay with IC50 greater than 50 μM.	42748754

In Vitro

Anti-cancerApoptosisCell Cycle RegulationEndoplasmic Reticulum Stress

Anti-cancer

SH458 (72 h) inhibited the proliferation of MDA-MB-231, MDA-MB-468, SUM149T, and 4T1 TNBC cells with IC₅₀ values of 0.14-0.28 μM, whereas the IC₅₀ values in normal MCF10A and HPNE cells were >50 μM^[1].
SH458 (0.03-3 μM; 7-10 days) selectively inhibited the clonogenic ability of MDA-MB-231 and MDA-MB-468 cells, showing potent inhibition at 0.1 μM, almost complete inhibition at 0.3 μM, while having no effect on MCF10A cells at 3 μM^[1].

Anti-cancer

Apoptosis

SH458 (1 μM; 24 h) induced apoptosis in MDA-MB-231 and MDA-MB-468 cells, with a total apoptosis rate of approximately 45.5%^[1].
SH458 (0.13-2 μM; 24 h) activates apoptosis and DNA damage checkpoint signaling in MDA-MB-231 and MDA-MB-468 cells, increasing C-PARP, C-Caspase 3, γH2AX, and CHK1/CHK2 phosphorylation while decreasing Cyclin B1^[1].

Anti-cancer

Cell Cycle Regulation

SH458 (0.125-1 μM; 24 h) induced G2/M phase cell cycle arrest in MDA-MB-231 and MDA-MB-468 cells^[1].

Endoplasmic Reticulum Stress

SH458 (0-2 μM; 0-24 h) activates UPR signaling in MDA-MB-231 and MDA-MB-468 cells, increasing p-IRE1α and p-eIF2α in a concentration- and time-dependent manner^[1].

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

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231 and MDA-MB-468 cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Induced apoptosis in both MDA-MB-231 and MDA-MB-468 cells in a dose-dependent manner.
At 1 μM, total apoptotic rates reached 45.48% and 45.50%, respectively, representing approximately an 8-fold increase compared with controls.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 and MDA-MB-468 cells
Concentration:

0, 0.125, 0.25, 0.5, 1, 2 μM (concentration course); 1 μM (time course)
Incubation Time:

24 h (concentration course); 0, 3, 6, 12, 24 h (time course)
Result:

Markedly increased phosphorylation levels of eIF2α and IRE1α in both concentration- and time-dependent manners in MDA-MB-231 and MDA-MB-468 cells.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-t	AUC_0-∞	V_z	CL	T_1/2	F
Mice^[1]	1.0 mg/kg	i.v.	0.083 h	173 ng/mL	124 ng·h/mL	132 ng·h/mL	17,500 mL/kg	141 mL/min/kg	2.20 h	/
Mice^[1]	10.0 mg/kg	p.o.	0.50 h	153 ng/mL	218 ng·h/mL	226 ng·h/mL	/	/	1.63 h	17.6 %

In Vivo

Anti-cancer

SH458 (10-20 mg/kg; i.p.; every 3 days) significantly inhibits MDA-MB-231 xenograft tumor growth with greater efficacy than Doxorubicin (HY-15142A)^[1].

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

Animal Model:

BALB/c nude (female, 4-5-week-old)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

i.p.; every 3 days
Result:

SH458 significantly suppressed tumor growth at both 10 and 20 mg/kg compared with the control group and showed greater antitumor efficacy than DOX.
Tumor weights in the SH458-treated groups were markedly lower than those in both the control and DOX groups.
Immunohistochemistry showed that SH458 markedly reduced Ki67 expression in tumor tissues.
SH458 significantly inhibited tumor growth in a dose-dependent manner.

Related Protocols :

Chemical Information

CAS. Nr. 3109470-77-8
Molecular Weight 458.55
Formel C₂₈H₃₀N₂O₄
SMILES

O=C(C1=CN=CC=C1)O[C@H]2CC[C@@]3([H])[C@]4([H])C(C=C5C(C)(C)C(C(C#N)=C[C@]5(C)[C@@]4([H])CC[C@@]32C)=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

Handling Instructions (2659 KB)

Verweise

[1]. Zhang JZ, et al. Synthesis and biological evaluation of cyanoenone- and enone-fused 4-androstene-3,17-dione derivatives against triple-negative breast cancer. Bioorganic chemistry. 2026 Sep 13;182:110487.

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.

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MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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SH458

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