Cat. No.: HY-200492

SU086

SU086 is a chalcone-derived HSP90 inhibitor. SU086 interacts with HSP90, reduces HSP90 protein levels, and suppresses glycolysis in prostate cancer cells. SU086 can be used in research related to advanced prostate cancer and castration-resistant prostate cancer (CRPC).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 1017898-53-1
Formule: C₁₈H₁₇NO₆
Masse moléculaire:343.33

Stockage:

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

SU086 Chemical Structure

CAS No.: 1017898-53-1

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Use of MCE Products

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform HSP :

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	IC50	2.024 μM	Inhibition of cell viability against human DU145 prostate cancer cells incubated for 72 hrs by CellTiter-Blue assay. Inhibition of cell viability against human DU145 prostate cancer cells incubated for 72 hrs by CellTiter-Blue assay.	35243415
LNCaP	IC50	2.128 μM	Inhibition of cell viability against human LNCaP prostate cancer cells incubated for 72 hrs by CellTiter-Blue assay. Inhibition of cell viability against human LNCaP prostate cancer cells incubated for 72 hrs by CellTiter-Blue assay.	35243415
LNCaP C4-2	IC50	3.027 μM	Inhibition of cell viability against human C4-2 prostate cancer cells incubated for 72 hrs by CellTiter-Blue assay. Inhibition of cell viability against human C4-2 prostate cancer cells incubated for 72 hrs by CellTiter-Blue assay.	35243415
PC-3	IC50	3.218 μM	Inhibition of cell viability against human PC-3 prostate cancer cells incubated for 72 hrs by CellTiter-Blue assay. Inhibition of cell viability against human PC-3 prostate cancer cells incubated for 72 hrs by CellTiter-Blue assay.	35243415

In Vitro

SU086 (compound 3b) (10 μM; 48 h) broadly inhibits cancer cell growth in the NCI-60 cell line screening, resulting in complete growth inhibition in 28 out of 59 evaluable cell lines, and a growth inhibition rate exceeding 90% in 44 cell lines; the growth of both DU145 and PC3 prostate cancer cells is completely suppressed^[1].
SU086 (72 h) reduces the viability of DU145, LNCaP, C4-2, PC-3 and 22Rv1 prostate cancer cells, with IC₅₀ values of 2.024, 2.128, 3.027, 3.218 and 8.304 μM, respectively^[1].
SU086 (1 μM; 6 days) inhibits the proliferation of C4-2, DU145 and 22Rv1 cells and reduces the number of viable cells in each cell line^[1].
SU086 (1 μM; 9 days) reduces the colony formation rate of C4-2, DU145, and 22Rv1 cells^[1].
SU086 (1 μM; 15 days) inhibits the growth of prostate cancer tumoroids derived from LuCaP 136 and LuCaP 147 PDX and reduces the tumoroid coverage area^[1].
SU086 (1 μM; 72 h pretreatment + 20 h) inhibits Transwell migration in C4-2, DU145, and 22Rv1 cells^[1].
SU086 (1 μM; 72 h pretreatment + 20 h) inhibits Matrigel Transwell invasion in C4-2, DU145 and 22Rv1 cells^[1].
SU086 (1 μM; 6 days) reduces the migration distance of C4-2 and DU145 cells from the Matrigel edge in the 3D Matrigel drop model^[1].
SU086 (5 μM; 72 h) reduces the Ki67 proliferation index from approximately 30% to below 5% in primary human prostate cancer tissue sections^[1].
The combination of SU086 (250 nM) and Enzalutamide (HY-70002) (5 μM) exhibits a synergistic effect in C4-2 cells, with a CDI of 0.672, and further inhibits colony formation; the combination of SU086 and Abiraterone (HY-70013) (2.5 μM) shows an additive effect, with a CDI of 1.022, and also further inhibits colony formation^[1].
SU086 (5 μM; 72 h) increases the level of cleaved caspase-3 in primary human prostate cancer tissue slices^[1].
SU086 (2.5 μM; 1.5 h) shifts the HSP90 melting curve by 17.31°C toward higher temperatures in the CETSA assay of DU145 cells, which supports the intracellular interaction between SU086 and HSP90^[1].
SU086 (1 μM; 24 or 48 h) reduces the protein level of HSP90 in C4-2 and DU145 cells; MG132 (HY-13259) (10 μM) partially reverses the SU086-induced downregulation of HSP90 ^[1].
SU086 (1 μM; 48 h) reduces the levels of 38 common proteins by more than 2-fold in C4-2 and DU145 cells, including HSP90, and enriches HSP90-interacting proteins and glycolysis-regulating proteins^[1].
SU086 (1 μM; 24 h) reduces glycolytic flux by approximately 50% and glycolytic capacity by 30%-50% in C4-2 and DU145 cells, while the OCR that reflects oxidative phosphorylation remains unchanged^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

NCI-60 panel
Concentration:

10 μM
Incubation Time:

48 h
Result:

Produced complete growth inhibition in 28 of 59 evaluable cancer cell lines.
Produced greater than 90% growth inhibition in 44 of 59 evaluable cancer cell lines.
Completely inhibited growth of DU145 and PC3 prostate cancer cells.

Cell Viability Assay^[1]

Cell Line:

LNCaP, C4-2, 22RV1, DU145, and PC-3 prostate cancer cells
Concentration:

0.625-10 μM
Incubation Time:

72 h
Result:

Inhibited cell viability with IC₅₀ values of 2.024 μM (DU145), 2.128 μM (LNCaP), 3.027 μM (C4-2), 3.218 μM (PC-3), and 8.304 μM (22RV1).

Cell Proliferation Assay^[1]

Cell Line:

C4-2, DU145, and 22RV1 prostate cancer cells
Concentration:

1 μM
Incubation Time:

6 days
Result:

Reduced viable cell numbers in C4-2, DU145, and 22Rv1 cells compared with vehicle.
Inhibited proliferation across AR-positive and AR-negative CRPC cell models.

Cell Proliferation Assay^[1]

Cell Line:

C4-2, DU145, and 22RV1 prostate cancer cells
Concentration:

1 μM
Incubation Time:

9 days
Result:

Drastically reduced colony formation rate in all three cell lines, with near-complete inhibition observed in C4-2 cells.

Cell Migration Assay ^[1]

Cell Line:

C4-2, DU145, and 22RV1 prostate cancer cells
Concentration:

1 μM
Incubation Time:

72 h pretreatment, then 20 h continued treatment
Result:

Reduced the number of migrated C4-2 cells.
Reduced the number of migrated DU145 cells.
Reduced the number of migrated 22Rv1 cells.

Cell Invasion Assay^[1]

Cell Line:

C4-2, DU145, and 22RV1 prostate cancer cells
Concentration:

1 μM
Incubation Time:

72 h pretreatment, then 20 h continued treatment
Result:

Significantly reduced the number of invasive cells per field in all three cell lines.

Western Blot Analysis^[1]

Cell Line:

C4-2 and DU145 prostate cancer cells
Concentration:

1 μM
Incubation Time:

24 h, 48 h
Result:

Led to a decrease in HSP90 protein levels in both cell lines after 24 h and 48 h of incubation.
Co-treatment with the proteasomal inhibitor MG132 partially reversed this decrease.

Cell Proliferation Assay^[1]

Cell Line:

C4-2 prostate cancer cells
Concentration:

250 nM (SU086); 5 μM (enzalutamide); 2.5 μM (abiraterone)
Incubation Time:

9 days
Result:

In combination with enzalutamide showed synergistic activity (coefficient of drug interaction [CDI] = 0.672), while in combination with abiraterone showed additive activity (CDI = 1.022).
Both combinations dramatically attenuated colony formation compared to single-agent treatments.

Western Blot Analysis^[1]

Cell Line:

C4-2
Concentration:

SU086 1 μM; MG132 10 μM
Incubation Time:

2 or 4 h
Result:

Decreased HSP90 protein levels after SU086 exposure.
Partially restored HSP90 levels when MG132 was combined with SU086.

In Vivo

SU086 (50 mg/kg; i.p.; once daily) inhibits the growth of C4-2 prostate cancer subcutaneous xenografts in male NSG mice and reduces the tumor Ki67 proliferation index, while not causing significant body weight changes^[1].
SU086 (50 mg/kg; i.p.; once daily) inhibits the growth of DU145 prostate cancer xenografts in male NSG mice, reduces Ki67 and vimentin levels, and increases E-cadherin and cleaved caspase-3 levels, while not causing significant changes in body weight^[1].
SU086 (50 mg/kg; i.p.; once daily; 18 days) prevents continuous tumor growth in the LuCaP 147 PDX model of male NSG mice bearing testosterone implants, reduces Ki67 and vimentin, increases E-cadherin, and no measurable toxicity is observed ^[1].
SU086 (50 mg/kg; i.p.; once daily; 18 days) delays the growth of LuCaP 136 PDX tumors in male NSG mice bearing testosterone implants, downregulates Ki67, vimentin and AR, and increases E-cadherin^[1].
SU086 (50 mg/kg; i.p.; once daily) reduces the lactate/pyruvate ratio in C4-2 and DU145 xenograft tumors; the median/average ratio in C4-2 tumors decreases from 111.7/121.9 to 101.8/112.3, and that in DU145 tumors decreases from 80.6/94.7 to 55.6/57.2^[1].
The combination of SU086 (50 mg/kg; i.p.; once daily) and Enzalutamide (10 mg/kg; oral gavage; once daily) for 21 days prevents the continuous growth of C4-2 xenograft tumors and significantly reduces the Ki67 proliferation index, with no observed abnormalities in body weight, liver histology, or kidney histology^[1].
The combination of SU086 (50 mg/kg; i.p.; once daily) and Abiraterone (200 mg/kg; oral gavage; once daily) for 21 days prevents the continuous growth of C4-2 xenograft tumors and significantly reduces the Ki67 proliferation index, with no obvious toxicity observed^[1].

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

Animal Model:

NOD-SCID-IL2Rγ-null (NSG) (male; testosterone-supplemented; subcutaneous patient-derived xenograft of LuCaP 136 metastatic prostate cancer cells)^[1]
Dosage:

50 mg/kg
Administration:

i.p., once daily for 18 days
Result:

Delayed LuCaP 136 tumor growth.
Reduced the Ki67 proliferation index.
Decreased vimentin.
Increased E-cadherin.
Decreased AR in AR-positive LuCaP 136 tumors.

Animal Model:

Male NSG mice bearing LuCaP 147 PDXs and supplemented with testosterone pellets^[1]
Dosage:

50 mg/kg
Administration:

i.p., once daily for 18 days
Result:

Halted further LuCaP 147 tumor growth.
Reduced the Ki67 proliferation index.
Decreased vimentin.
Increased E-cadherin.
Produced no measurable toxicity.

Animal Model:

Male NSG mice bearing C4-2 xenografts^[1]
Dosage:

SU086 50 mg/kg + enzalutamide 10 mg/kg
Administration:

i.p., once daily; enzalutamide: oral gavage, once daily; 21 days
Result:

Halted further tumor growth throughout the 21-day administration period.
Markedly reduced the Ki67 proliferation index.
Produced no measurable body-weight changes or liver/kidney histological abnormalities.

Animal Model:

Male NSG mice bearing C4-2 xenografts^[1]
Dosage:

SU086 50 mg/kg + abiraterone 200 mg/kg
Administration:

i.p., once daily; abiraterone: oral gavage, once daily; 21 days
Result:

Halted further tumor growth throughout the 21-day administration period.
Markedly reduced the Ki67 proliferation index.
Produced no measurable toxicity.

Chemical Information

CAS No. 1017898-53-1
Masse moléculaire 343.33
Formule C₁₈H₁₇NO₆
SMILES

O=C(C1=C(C=C(C=C1OC)OC)OC)/C=C/C2=CC([N+]([O-])=O)=CC=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Rice MA, et al. SU086, an inhibitor of HSP90, impairs glycolysis and represents a treatment strategy for advanced prostate cancer. Cell reports. Medicine. 2022 Feb 15;3(2):100502.

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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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SU086

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