2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. Onalespib lactate

Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC).

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CAS No. : 1019889-35-0

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Onalespib lactate Related Antibodies

Top Publications Citing Use of Products

    Onalespib lactate purchased from MedChemExpress. Usage Cited in: J Labelled Comp Radiopharm. 2025 Apr;68(4):e4144.  [Abstract]

    In vitro autoradiography study. Slices were incubated with [18F]FEHSP990 (11 kBq/mL). Binding specificity was assessed by preincubation with authentic reference compound (FEHSP990), homologous (HSP990) and heterologous (Onalespib, PU‐H71) inhibitors (10 μM; 10 min) at RT. Rat brain slices (n = 3 per preincubation condition) and U87 tumour slices (n = 3 per preincubation condition).

    Onalespib lactate purchased from MedChemExpress. Usage Cited in: J Labelled Comp Radiopharm. 2025 Apr;68(4):e4144.  [Abstract]

    In vitro cell binding study. U87 cells were incubated with [18F]FEHSP990 (84 kBq/mL). Binding specificity was assessed by preincubation with homologous (HSP990) and heterologous (Onalespib, PU‐H71) inhibitors (100 μM; 60 min) at 37°C (n = 3 per preincubation condition).

    Onalespib lactate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201.  [Abstract]

    5637 and SV-HUC cells (1 × 104 per well) were evenly distributed in 96-well plates overnight. Cells were incubated with AUY922 (10 nM), ganetespib (10 nM), SNX2112 (100 nM), or AT13387 (Onalespib) (100 nM) for 48 h. For the caspase 3/7 assay, the HSP90 inhibitor-treated 5637 or SV-HUC cells are stained with Nexcelom ViaStain Caspase 3/7 reagent and Hoechst 33342. Caspase 3/7 positive cells are identified using the Celigo imaging cytometer, and the percentage of apoptotic caspase 3/7 positive cells is calculated with the Celigo software.

    Onalespib lactate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201.  [Abstract]

    Heat shock protein 90 (HSP90) inhibitors suppress cell growth and proliferation in human bladder carcinoma cells. 5637 cells were evenly distributed in 96-well plates (5 × 103 cells/well) and treated for 72 h with AUY922, ganetespib (STA9090), SNX2112, AT13387 (Onalespib), or CUDC395 at the indicated concentrations. The ability of HSP90 inhibitors to inhibit cell growth and proliferation was determined by the MTS assay.

    Onalespib lactate purchased from MedChemExpress. Usage Cited in: J Appl Toxicol. 2017 Nov;37(11):1325-1332.  [Abstract]

    Alleviation of graphene toxicity by using chemical inhibitors (Onalespib (AT13387 et al; 20 nM pretreatment 2 h)) after 48 h exposure of NRK-52E cells with graphene (50 μg/ml). Quantification of TUNEL-positive cells in NRK-52E cells treated with graphene in the presence of chemical inhibitors for HO-1, HSP90, caspase 3, DNase I and EndoG (p < 0.01 for all bars vs. Gn).

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    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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    Description

    Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC)[1][2][3][4].

    IC50 & Target[4]

    HSP90

    0.71 nM (Kd)

    In Vitro

    Onalespib lactate (0-0.4 µM; 72 h, 48 h) inhibits the proliferation, survival and migration of glioma cells[2].
    Onalespib lactate (0-0.4 µM; 48 h) decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein in a dose-dependent manner[2].

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

    Onalespib lactate Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: LN229, U251 and A172 cells
    Concentration: 0.1, 0.2, 0.4 µM
    Incubation Time: 72 h
    Result: Inhibited cell proliferation in a dose-dependent manner.

    Western Blot Analysis[2]

    Cell Line: LN229, U251 and A172 cells
    Concentration: 0.1, 0.2, 0.4 µM
    Incubation Time: 48 h
    Result: Decreased the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein in a dose-dependent manner.
    In Vivo

    Onalespib lactate (30 mg/kg; i.v.; once) crosses the blood-brain barrier (BBB) and causes sustained inhibition of HSP90 in 6-week-old ICR mice[2].
    Onalespib lactate (0.5 µM; from 5 to 10 days post-transplant) and TMZ (10 µM) reduce tumor growth and extend survival in zebrafish embryos[2].
    Onalespib lactate (5, 10 mg/kg for HCT116 xenografts, 20 mg/kg for A431 xenografts; i.p.; daily for 3 days) shows anti-tumor activity in HCT116 and A431 xenografts[3].

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

    Animal Model: Female nu/nu Balb/c mice (HCT116 and A431 xenografts)[3]
    Dosage: 5, 10 mg/kg for HCT116 xenografts, 20 mg/kg for A431 xenografts
    Administration: I.p.; on day 1, 2, and 3 days
    Result: Inhibited tumor growth and had a median survival of 9.5 days and the maximum survival was 14 days in HCT116 xenografts, reduced the tumor size significantly by 32% in A431 xenografts.
    Molecular Weight

    499.60

    Formula

    C27H37N3O6
    CAS No.
    SMILES

    C[C@H](O)C(O)=O.O=C(N1CC2=C(C=C(CN3CCN(C)CC3)C=C2)C1)C4=CC(C(C)C)=C(O)C=C4O
    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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    Onalespib lactate Related Classifications

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    • 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:

    Onalespib1019889-35-0AT13387AT 13387AT-13387HSPHeat shock proteinscross the blood-brain barrierantitumorproliferationmigrationLN229U251A172 cellsEGFRInhibitorinhibitorinhibit

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