GLPBio

HA15

Catalog No.: GC19188Purity:>99.50%
COASDSData Sheet
HA15 is a molecule that specifically targets BiP/GRP78/HSPA5, binding to and inhibiting its ATPase activity, which leads to the dissociation of BiP from PERK, IRE1α, and ATF6, thereby triggering endoplasmic reticulum stress.

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HA15
Cas No.: 1609402-14-3
5mgIn Stock
$52.00
1
10mgIn Stock
$74.00
1
50mgIn Stock
$235.00
1
100mgIn Stock
$402.00
1
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Description

HA15 is a molecule that specifically targets BiP/GRP78/HSPA5, binding to and inhibiting its ATPase activity, which leads to the dissociation of BiP from PERK, IRE1α, and ATF6, thereby triggering endoplasmic reticulum stress[1][2][3]. HA15 has demonstrated anti-tumor effects in a variety of human cancers, including melanoma, breast, pancreas, and adrenocortical carcinoma[2].

HA15 (1-10μM, 24h) decreases melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO), with an IC50 of 1-2.5μM in A375 cells[1]. HA15 (10μM, 48h) induces typical dilated endoplasmic reticulum cisternae in A375 cells[1]. HA15 (1, 5 and 10μM; 48h) induces apoptosis in A375 cells by increasing the levels of the cleaved and activated form of caspase 9 and decreasing the levels of the zymogenic form of caspase 3[1].

HA15 (0.7mg/mouse, 5 days/week, 5 weeks, i.p.) treatment delayed tumor growth in malignant pleural mesothelioma (MPM) mouse model[2]. HA15 (0.5mg/kg twice weekly, 3 weeks, i.p.) in combination with BTZ, was more effective at inhibiting tumor growth than BTZ alone in a multiple myeloma mouse model[4].

References:
[1] Cerezo M, Lehraiki A, Millet A, et al. Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance. Cancer Cell. 2016 Jun 13;29(6):805-819.
[2] Xu D, Yang H, Yang Z, et al. Endoplasmic Reticulum Stress Signaling as a Therapeutic Target in Malignant Pleural Mesothelioma. Cancers (Basel). 2019 Oct 8;11(10):1502.
[3] Ruggiero C, Doghman-Bouguerra M, Ronco C, et al. The GRP78/BiP inhibitor HA15 synergizes with mitotane action against adrenocortical carcinoma cells through convergent activation of ER stress pathways. Mol Cell Endocrinol. 2018 Oct 15;474:57-64.
[4] Chen Y, Tao Y, Hu K, et al. GRP78 inhibitor HA15 increases the effect of Bortezomib on eradicating multiple myeloma cells through triggering endoplasmic reticulum stress. Heliyon. 2023 Sep 2;9(9):e19806.

Protocol

Cell experiment [1]:

Cell lines

Resistant melanoma cell lines A375

Preparation Method

A375 cells were treated with indicated concentrations (1-10μM) of HA15. After 24h, viable cells were counted using the trypan blue dye exclusion method.

For trypan blue staining, 200μl of cells was aseptically transferred to a 1.5ml clear Eppendorf tube and incubated for 3min at room temperature with an equal volume of 0.4% trypan blue solution. Viable cells were counted and the results are expressed as the percentage of the value of control cells.

Reaction Conditions

1-10μM, 24h

Applications

HA15 decreases melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO), with an IC50 of 1-2.5μM in A375 cells.
Animal experiment [2]:

Animal models

Malignant pleural mesothelioma (MPM) mouse model

Preparation Method

Suspensions of tumor cells (in PBS) mixed with 1:1 with BD Matrigel Basement Membrane Matrix were subcutaneously inoculated in left and right flanks (BE261T cells: 1×106/injection). When tumors were palpable, mice were randomly assigned to treatment groups: (1) control; (2) Cisplatin (3.75mg/kg) plus Pemetrexed (83mg/kg) (i.p., once weekly) for five weeks; (3) HA15 (0.7mg/mouse, i.p., 5 days/week) for five weeks. Mice weight and tumor size were measured every three days. Tumor size was calculated as follows: (length × width × width)/2. At the endpoint, blood samples were collected through cardiac puncta and subjected to the determination of transaminase activities.

Dosage form

0.7mg/mouse, 5 days/week, 5 weeks, i.p.

Applications

HA15 treatment delayed tumor growth in patient-derived xenograft models compared to the vehicle treatment.

References:
[1] Cerezo M, Lehraiki A, Millet A, et al. Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance. Cancer Cell. 2016 Jun 13;29(6):805-819.
[2] Xu D, Yang H, Yang Z, et al. Endoplasmic Reticulum Stress Signaling as a Therapeutic Target in Malignant Pleural Mesothelioma. Cancers (Basel). 2019 Oct 8;11(10):1502.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1609402-14-3
SMILES
CC(NC1=NC(C2=CC=CC(NS(=O)(C3=C4C=CC=C(N(C)C)C4=CC=C3)=O)=C2)=CS1)=O
Molecular Formula
C23H22N4O3S2
Molecular Weight
466.58
Solubility
DMSO : ≥ 50 mg/mL (107.16 mM);Water : < 0.1 mg/mL (insoluble)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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