2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP CDK
  4. Hsp90-IN-46

Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer.

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Hsp90-IN-46

Hsp90-IN-46 Chemical Structure

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Hsp90-IN-46 Related Antibodies

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Description

Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer[1].

IC50 & Target[1]

HSP90

 

In Vitro

Hsp90-IN-46 (Compound 13b) (0.01-100 μM; 48 h) exhibits potent, broad-spectrum anticancer activity across 48 human tumor cell lines, with a GI50 value range of 2.17 to 9.60 μM. It achieves total growth inhibition in 26 cell lines and shows extremely low lethality to most cell lines in assays with 5 concentrations applied for 48 h[1].
Hsp90-IN-46 (48 h) exhibits highly active and selective inhibitory effects on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 1.33 μM and 1.95 μM, respectively[1].
Hsp90-IN-46 (1-5 μM, 9 days) inhibits the proliferation of MDA-MB-231 breast cancer cells, reduces the expression of the proliferation marker Ki67 in MCF-7 and MDA-MB-231 breast cancer cells, and downregulates the expression of Hsp90 substrate oncoproteins HER2 and CDK4[1].
Hsp90-IN-46 directly inhibits the activity of Hsp90 in an in vitro AlphaLISA-based assay with an IC50 of 12.397 μM, and potently inhibits Hsp90 ATPase activity in a coupled spectrophotometric assay with an IC50 of 0.986 μM[1].
Hsp90-IN-46 (10 μM) induces a moderate heat shock response in HEK-293 cells, increasing the expression level of HspA1A mRNA by 8.7-fold at a concentration of 10 μM[1].

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

Hsp90-IN-46 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: 48 human tumor cell lines from multiple subpanels (NSCLC, colon, CNS, melanoma, ovarian, renal, prostate, leukemia, breast)
Concentration: 10 μM
Incubation Time: 48 h
Result: Exhibited a mean growth inhibition (GI%) of 78.84% across 48 cell lines.
Showed strong cytotoxicity (GI% 57.74-68.93%) against NSCLC (NCI-H226), colon (HCC-2998, HT29, SW-620), CNS (SF-539), melanoma (M14), ovarian (OVCAR-3, OVCAR-8), renal (A498, RXF 393), and prostate (DU-145) cancer cell lines.
Demonstrated potent cytotoxicity (GI% 70.24-97.44%) against all leukemia cell lines and most NSCLC, melanoma, colon, CNS, ovarian, renal, and breast cancer cell lines.
Induced 56.97% and 4.33% lethality against melanoma SK-MEL-5 and SK-MEL-2 cell lines, respectively.

Cell Cytotoxicity Assay[1]

Cell Line: 60 human tumor cell lines
Concentration: 0.01-100 μM
Incubation Time: 48 h
Result: Demonstrated potent cytotoxicity with GI50 values of 2.17-9.60 μM against 48 cell lines.
Showed lower activity with GI50 values of 10.20-22.70 μM against 12 cell lines.
Induced total growth inhibition (TGI) with values of 6.23-91.00 μM against 26 cell lines (including breast MDA-MB-468, melanoma SK-MEL-5, UACC-62, SK-MEL-2, and ovarian OVCAR-3).
Exhibited minimal toxicity with LC50 >92.5 μM against 57 cell lines, except LC50 values of 27.40-61.30 μM against colon COLO 205 and melanoma SK-MEL-5, UACC-62 cell lines.
Achieved a full-panel GI50 mean graph-midpoint (MG-MID) value of 5.89 μM, with breast cancer MDA-MB-468 as the most sensitive cell line (GI50 = 2.17 μM) and ovarian cancer OVCAR-5 as the least sensitive (GI50 = 22.7 μM).

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7, MDA-MB-231, Caco-2, A549 cancer cell lines; normal human skin fibroblast (HSF) cells
Concentration: Serial concentrations
Incubation Time: 48 h
Result: Displayed IC50 values of 1.33 μM (MCF-7), 1.95 μM (MDA-MB-231), 4.62 μM (Caco-2), 11.89 μM (A549), and 46.96 μM (HSF).
Achieved selectivity index values of 35.31 (MCF-7), 24.08 (MDA-MB-231), 10.16 (Caco-2), and 3.95 (A549).

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 5 μM
Incubation Time: 9 days
Result: Significantly reduced colony formation from 173 colonies per well (control) to 91 colonies per well.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC
Rat[1] 50 mg/kg i.p. 6.74 ± 1.28 μM 1 h 2.98 h 30.68
In Vivo

Hsp90-IN-46 (13b) (50 mg/kg; i.p.; daily; 6 consecutive days) exhibits significant anti-tumor activity in a triple-negative breast cancer tumor xenograft mouse model[1].

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

Animal Model: BALB/c mice (immunocompromised)[1]
Dosage: 50 mg/kg
Administration: i.p.; daily; 6 consecutive days
Result: Reduced MDA-MB-231 xenograft tumor volume and tumor weight by approximately 33%.
Reduced EGFR expression in tumor sections to 0.17-0.92% reaction area.
Maintained stable body weight in treated mice.
Molecular Weight

468.30

Formula

C21H18BrN5O3
SMILES

C/C(NC1=CC=CC=C1NC(/C(C#N)=N/NC2=CC=C(Br)C=C2)=O)=C3C(OCC/3)=O
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
References
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Hsp90-IN-46 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-46HSPCDKHeat shock proteinsCyclin dependent kinaseHsp90 inhibitortriple-negative breast cancerleukemianon-small cell lung cancercolon cancerovarian cancerrenal cancerprostate cancerbreast cancerMCF-7 cellsMDA-MB-231 cellsBALB/c miceInhibitorinhibitorinhibit

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