2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Autophagy Apoptosis
  3. HSP Autophagy Apoptosis
  4. HA15

HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.

For research use only. We do not sell to patients.

HA15 Chemical Structure

HA15 Chemical Structure

CAS No. : 1609402-14-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 84 In-stock
Solution
10 mM * 1 mL in DMSO USD 84 In-stock
Solid
5 mg USD 82 In-stock
10 mg USD 132 In-stock
25 mg USD 250 In-stock
50 mg USD 375 In-stock
100 mg USD 562 In-stock
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Customer Review

Based on 28 publication(s) in Google Scholar

HA15 Related Antibodies

Top Publications Citing Use of Products

    HA15 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2020 Jun 30;10(1):10604.  [Abstract]

    HA15, a GRP78 inhibitor, to inhibit GRP78, and finds that inhibition of GRP78 abolished the downregulation of Col1 and α-SMA in response to UCHL1 siRNA in CFs with TGF-β1 stimulation.

    View All HSP Isoform Specific Products:

    View All Isoforms
    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity[1].

    IC50 & Target

    BiP/GRP78/HSPA5[1]
    In Vitro

    HA15 (10 μM; 1-24 hours) induces an early endoplasmic reticulum stress (ER Stress)[1].
    HA15 (0-10μM; 24 hours) decreases melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO), with an IC50 of 1-2.5 μM in A375 cells[1].
    HA15 (1-10 μM; 24 hours) induces apoptosis in A375 cells[1].
    HA15 (1-24 μM; 24 hours) induces autophagy[1].
    HA15 (10 μM; 48 hours) has high efficiency in inducing cell death and ER stress in BRAF-inhibitor-resistant melanoma cells. And HA15 inhibits tumor growth through autophagic and apoptotic mechanisms initiated by ER stress[1].
    No deleterious effects on the viability of normal human melanocytes or human fibroblasts were observed with low or high doses of HA15[1].

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

    HA15 Related Antibodies

    Cell Viability Assay[1]

    Cell Line: A375 cells
    Concentration: 1 μM,2.5 μM,5 μM,7.5 μM,10 μM
    Incubation Time: 24 hours
    Result: Decreased melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO) in A375 cells.

    Apoptosis Analysis[1]

    Cell Line: A375 cells
    Concentration: 1 μM, 5 μM, 10 μM
    Incubation Time: 24 hours
    Result: Induces apoptosis.

    Cell Autophagy Assay[1]

    Cell Line: A375 cells
    Concentration: 1 μM, 4 μM, 10 μM, 24 μM
    Incubation Time: 24 hours
    Result: Increased LC3B-II expression after 1 hour and persisted after 24 hours, enhanced the expression level of Beclin 1, clearly be indicated that induces autophagy.

    Western Blot Analysis[1]

    Cell Line: A375 cells
    Concentration: 10 μM
    Incubation Time: 1 hour, 4 hours, 10 hours, 24 hours
    Result: Exhibited a rapid induction within 1 hour of the ER stress markers (phosphorylation of PERK and elF2α and a weak increase in ATF4 and CHOP expression)
    In Vivo

    HA15 (0.7 mg/mouse/day; i.h.; over 2 weeks) inhibits melanoma tumor development in mice, induces no apparent toxicity and no change in their behavior, body mass, or liver mass, suggesting an absence of hepatomegaly[1].
    HA15 (0.7 mg/mouse; i.p.; 5 days/week) suppresses MPM tumor growth in vivo[3].

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

    Animal Model: 6-weeks female BALB/c nu/nu (nude) mice with A375 melanoma cells xenograft[1]
    Dosage: 0.7 mg/mouse/day
    Administration: Subcutaneous injection; over a period of 2 weeks
    Result: Attenuated the development of tumors.
    Animal Model: Mouse, NSG (NOD-scid IL2Rγnull)[3]
    Dosage: 0.7 mg/mouse
    Administration: Intraperitoneal injection, 5 days/week, for 5 weeks
    Result: Suppressed MPM tumor growth.
    Molecular Weight

    466.58

    Formula

    C23H22N4O3S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    CC(NC1=NC(C2=CC=CC(NS(=O)(C3=C4C=CC=C(N(C)C)C4=CC=C3)=O)=C2)=CS1)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (107.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1433 mL 10.7163 mL 21.4326 mL
    5 mM 0.4287 mL 2.1433 mL 4.2865 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.98%

    COA (253 KB) RP-HPLC (242 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1433 mL 10.7163 mL 21.4326 mL 53.5814 mL
    5 mM 0.4287 mL 2.1433 mL 4.2865 mL 10.7163 mL
    10 mM 0.2143 mL 1.0716 mL 2.1433 mL 5.3581 mL
    15 mM 0.1429 mL 0.7144 mL 1.4288 mL 3.5721 mL
    20 mM 0.1072 mL 0.5358 mL 1.0716 mL 2.6791 mL
    25 mM 0.0857 mL 0.4287 mL 0.8573 mL 2.1433 mL
    30 mM 0.0714 mL 0.3572 mL 0.7144 mL 1.7860 mL
    40 mM 0.0536 mL 0.2679 mL 0.5358 mL 1.3395 mL
    50 mM 0.0429 mL 0.2143 mL 0.4287 mL 1.0716 mL
    60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8930 mL
    80 mM 0.0268 mL 0.1340 mL 0.2679 mL 0.6698 mL
    100 mM 0.0214 mL 0.1072 mL 0.2143 mL 0.5358 mL
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    HA15 Related Classifications

    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:

    HA151609402-14-3HA 15HA-15HSPAutophagyApoptosisHeat shock proteinsInhibitorinhibitorinhibit

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