HA15
Based on 33 publication(s) in Google Scholar
HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.98%
- No. CAS: 1609402-14-3
- Fòrmula: C23H22N4O3S2
- Peso molecular:466.58
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) HA15
More- Signal Transduct Target Ther. 2023 Mar 15;8(1):107. [Abstract]
- J Am Chem Soc. 2022 Jun 15;144(23):10407-10416. [Abstract]
- Adv Sci (Weinh). 2025 Jan;12(4):e2406674. [Abstract]
- Adv Healthc Mater. 2023 Oct;12(26):e2300913. [Abstract]
- Leukemia. 2023 Apr;37(4):843-853. [Abstract]
- Free Radic Biol Med. 2023 Nov 1:208:299-308. [Abstract]
- EMBO Mol Med. 2023 Nov 8;15(11):e17761. [Abstract]
- JCI Insight. 2023 Mar 22;8(6):e141110. [Abstract]
- Int J Mol Sci. 2024 May 17;25(10):5475. [Abstract]
- Sci Rep. 2024 May 6;14(1):10407. [Abstract]
- Sci Rep. 2020 Jun 30;10(1):10604. [Abstract]
- Neoplasia. 2024 Sep:55:101020. [Abstract]
- Neoplasia. 2022 Nov:33:100837. [Abstract]
- Cancers (Basel). 2019 Oct 8;11(10):1502. [Abstract]
- Mol Oncol. 2025 Jul 9. [Abstract]
- Biomedicines. 2021 Jan 20;9(2):96. [Abstract]
- FASEB J. 2023 Dec;37(12):e23274. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2021 Oct;1868(11):119101. [Abstract]
- Genes Immun. 2025 Apr 15. [Abstract]
- Bone. 2022 Jan:154:116262. [Abstract]
- Pathogens. 2021 Mar 2;10(3):283. [Abstract]
- Mol Immunol. 2023 Jun:158:79-90. [Abstract]
- Exp Cell Res. 2021 Sep 15;406(2):112781. [Abstract]
- Reprod Toxicol. 2022 Oct:113:103-109. [Abstract]
- Biochem Genet. 2025 May 23. [Abstract]
- Biol Open. 2020 Nov 12;9(11):bio053298. [Abstract]
- bioRxiv. 2026 Jan 19.
- bioRxiv. 2025 March 11.
- bioRxiv. 2024 August 21.
- Chemosphere. 2023 May:322:138195. [Abstract]
- Research Square Print. December 9th, 2022.
- Dis Markers. 2022 Jul 13:2022:7115181. [Abstract]
- bioRxiv. 2020 Mar.
Customer Validation & Images
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In Vivo Efficacy Study
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Flow Cytometry
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
Actividad biológica
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Grp78 |
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Cell Line
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Type | Value | Description | References |
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| A-375 | IC50 |
1 μM
Compound: 10; HA15
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Antitumor activity against human A-375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
Antitumor activity against human A-375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
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[PMID: 37690265] |
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.
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Cell Line:A375 cells
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Concentration:1 μM,2.5 μM,5 μM,7.5 μM,10 μM
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Incubation Time:24 hours
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Result:Decreased melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO) in A375 cells.
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Cell Line:A375 cells
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Concentration:1 μM, 5 μM, 10 μM
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Incubation Time:24 hours
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Result:Induces apoptosis.
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Cell Line:A375 cells
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Concentration:1 μM, 4 μM, 10 μM, 24 μM
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Incubation Time:24 hours
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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.
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Cell Line:A375 cells
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Concentration:10 μM
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Incubation Time:1 hour, 4 hours, 10 hours, 24 hours
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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)
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.
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Animal Model:6-weeks female BALB/c nu/nu (nude) mice with A375 melanoma cells xenograft[1]
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Dosage:0.7 mg/mouse/day
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Administration:Subcutaneous injection; over a period of 2 weeks
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Result:Attenuated the development of tumors.
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Animal Model:Mouse, NSG (NOD-scid IL2Rγnull)[3]
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Dosage:0.7 mg/mouse
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Administration:Intraperitoneal injection, 5 days/week, for 5 weeks
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Result:Suppressed MPM tumor growth.
Chemical Information
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No. CAS 1609402-14-3
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Appearance Solid
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Peso molecular 466.58
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Fòrmula C23H22N4O3S2
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Color Light yellow to green yellow
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SMILES
CC(NC1=NC(C2=CC=CC(NS(=O)(C3=C4C=CC=C(N(C)C)C4=CC=C3)=O)=C2)=CS1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (33)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
SIRT7 orchestrates melanoma progression by simultaneously promoting cell survival and immune evasion via UPR activation. [Abstract]2023 Mar 15;8(1):107. PMID: 36918544 -
J Am Chem Soc
Target Profiling of an Iridium(III)-Based Immunogenic Cell Death Inducer Unveils the Engagement of Unfolded Protein Response Regulator BiP. [Abstract]2022 Jun 15;144(23):10407-10416. PMID: 35658433
HA15 purchased from MedChemExpress. Usage Cited in: J Am Chem Soc. 2022 Jun 15;144(23):10407-10416. [Abstract]
HA15 (1-100 μM) dampened the ATPase activity of BiP in HCT116 cells.
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Adv Sci (Weinh)
Hypoxia Induced Lnc191 Upregulation Dictates the Progression of Esophageal Squamous Cell Carcinoma by Activating GRP78/ERK Pathway. [Abstract]2025 Jan;12(4):e2406674. PMID: 39629920
HA15 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jan;12(4):e2406674. [Abstract]
HA15 (20 mg/kg; i.p.; once daily for 9 d) abrogated the increase in tumor volume and weight of ESCC in Balb/c nude mice induced by lnc191 overexpression.
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Adv Healthc Mater
Copper Increases the Sensitivity of Cholangiocarcinoma Cells to Tripterine by Inhibiting TMX2-Mediated Unfolded Protein Reaction Activation. [Abstract]2023 Oct;12(26):e2300913. PMID: 37119498
HA15 purchased from MedChemExpress. Usage Cited in: Adv Healthc Mater. 2023 Oct;12(26):e2300913. [Abstract]
HA15 (15 nM) inhibited the activation of the UPR and enhanced the toxicity of chemotherapeutic drugs in HuCCT1 cells.
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Leukemia
Human gene-engineered calreticulin mutant stem cells recapitulate MPN hallmarks and identify targetable vulnerabilities. [Abstract]2023 Apr;37(4):843-853. PMID: 36813992
HA15 purchased from MedChemExpress. Usage Cited in: Leukemia. 2023 Apr;37(4):843-853. [Abstract]
HA15 (5 µM; 12-14 d) selectively reduced CFU-GM and BFU-E colony formation in DEL mutant cells and significantly decreased CFU-Mk colony formation in both DEL and INS mutant cells.
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Free Radic Biol Med
Azoramide prevents MPP+-induced dopaminergic neuronal death via upregulating ER chaperone BiP expression. [Abstract]2023 Nov 1:208:299-308. PMID: 37625657 -
EMBO Mol Med
NRF3 suppresses squamous carcinogenesis, involving the unfolded protein response regulator HSPA5. [Abstract]2023 Nov 8;15(11):e17761. PMID: 37807968
HA15 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2023 Nov 8;15(11):e17761. [Abstract]
HA 15 (25 μM) significantly reduced the spheroid size of NRF3‐KO SCC13 cells.
HA15 purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2023 Nov 8;15(11):e17761. [Abstract]
HA15 (1.69 × 10−3 mg/ear; i.t.; every 2-3 days for 6 times) attenuated the growth of tumors in NOD/SCID mice formed by NRF3-KO HaCaT-Ras cells.
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JCI Insight
2023 Mar 22;8(6):e141110. PMID: 36802340 -
Int J Mol Sci
Molecular Characterization and Inhibition of a Novel Stress-Induced Mitochondrial Protecting Role for Misfolded TrkAIII in Human SH-SY5Y Neuroblastoma Cells. [Abstract]2024 May 17;25(10):5475. PMID: 38791513 -
Sci Rep
The interaction of GRP78 and Zika virus E and NS1 proteins occurs in a chaperone-client manner. [Abstract]2024 May 6;14(1):10407. PMID: 38710792 -
Sci Rep
Ubiquitin C-terminal hydrolase L1 (UCHL1) regulates post-myocardial infarction cardiac fibrosis through glucose-regulated protein of 78 kDa (GRP78). [Abstract]2020 Jun 30;10(1):10604. PMID: 32606430
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.
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Neoplasia
GRP78 inhibitor YUM70 upregulates 4E-BP1 and suppresses c-MYC expression and viability of oncogenic c-MYC tumors. [Abstract]2024 Sep:55:101020. PMID: 38991376 -
Neoplasia
Targeting GRP78 suppresses oncogenic KRAS protein expression and reduces viability of cancer cells bearing various KRAS mutations. [Abstract]2022 Nov:33:100837. PMID: 36162331 -
Cancers (Basel)
Endoplasmic Reticulum Stress Signaling as a Therapeutic Target in Malignant Pleural Mesothelioma. [Abstract]2019 Oct 8;11(10):1502. PMID: 31597321 -
Mol Oncol
Raphin-1 mediates the survival and sensitivity to radiation of pediatric-type diffuse high-grade glioma via phosphorylated eukaryotic initiation factor 2α-dependent and -independent processes. [Abstract]2025 Jul 9. PMID: 40632659 -
Biomedicines
Cell Proliferation Is Strongly Associated with the Treatment Conditions of an ER Stress Inducer New Anti-Melanoma Drug in Melanoma Cell Lines. [Abstract]2021 Jan 20;9(2):96. PMID: 33498201 -
FASEB J
GRP78 acts as a cAMP/PKA signaling modulator through the MC4R pathway in porcine embryonic development. [Abstract]2023 Dec;37(12):e23274. PMID: 37917004 -
Biochim Biophys Acta Mol Cell Res
Adipocyte-driven unfolded protein response is a shared transcriptomic signature of metastatic prostate carcinoma cells. [Abstract]2021 Oct;1868(11):119101. PMID: 34280426 -
Genes Immun
Comprehensive analysis of heat shock proteins in glioma revealed the association with glioma-associated myeloid cells. [Abstract]2025 Apr 15. PMID: 40234584 -
Bone
Suppressing phosphoinositide-specific phospholipases Cγ1 promotes mineralization of osteoarthritic subchondral bone osteoblasts via increasing autophagy, thereby ameliorating articular cartilage degeneration. [Abstract]2022 Jan:154:116262. PMID: 34813965 -
Pathogens
Proteomic Discovery of VEEV E2-Host Partner Interactions Identifies GRP78 Inhibitor HA15 as a Potential Therapeutic for Alphavirus Infections. [Abstract]2021 Mar 2;10(3):283. PMID: 33801554 -
Mol Immunol
HSPA5, as a ferroptosis regulator, may serve as a potential therapeutic for head and neck squamous cell carcinoma. [Abstract]2023 Jun:158:79-90. PMID: 37172353 -
Exp Cell Res
2021 Sep 15;406(2):112781. PMID: 34400174 -
Reprod Toxicol
2022 Oct:113:103-109. PMID: 35973673 -
Biochem Genet
GSDME Deficiency Suppresses ER Stress-Induced Autophagic Cell Death via mTOR/S6K1 Activation in Hepatobiliary Carcinomas. [Abstract]2025 May 23. PMID: 40407851 -
Biol Open
Targeted inhibition of GRP78 by HA15 promotes apoptosis of lung cancer cells accompanied by ER stress and autophagy. [Abstract]2020 Nov 12;9(11):bio053298. PMID: 33115703 -
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Chemosphere
Bisphenol C induces developmental defects in liver and intestine through mTOR signaling in zebrafish (Danio rerio). [Abstract]2023 May:322:138195. PMID: 36822516 -
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Dis Markers
2022 Jul 13:2022:7115181. PMID: 35872700 -
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Cerezo M et al. Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance. Cancer Cell. 2016 Jun 13;29(6):805-19. [Content Brief]
[2]. Ruggiero 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. [Content Brief]
[3]. Duo Xu, et al. Endoplasmic Reticulum Stress Signaling as a Therapeutic Target in Malignant Pleural Mesothelioma. Cancers (Basel). 2019 Oct; 11(10): 1502. [Content Brief]
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 |
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| 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 |
HA15 Related Classifications
HY-100437 Related Classifications
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