Art. -Nr.: HY-100437

HA15

Name: HA15
Brand: MedChemExpress
SKU: HY-100437
Price: 70.00 USD
Availability: InStock
Rating: 5 (33 reviews)

33 Cited Publications

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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.

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Reinheit: 99.98%
CAS. Nr.: 1609402-14-3
Formel: C₂₃H₂₂N₄O₃S₂
Molecular Weight:466.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

HA15 Chemical Structure

CAS. Nr.: 1609402-14-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (33)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Grp78

Alle HSP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1 μM Compound: 10; HA15	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	[PMID: 37690265]

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.

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.

Chemical Information

CAS. Nr. 1609402-14-3
Appearance Solid
Molecular Weight 466.58
Formel C₂₃H₂₂N₄O₃S₂
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (33)

All Bio/Physico-chemical AssayIn Vivo Efficacy StudyCell Proliferation/Viability AssayFlow CytometryWB

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Journal Impact Factor

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.
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.
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.
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.
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.
JCI Insight

Neutrophil extracellular traps contribute to coagulopathy after traumatic brain injury. [Abstract]

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.
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

HA15 alleviates bone loss in ovariectomy-induced osteoporosis by targeting HSPA5. [Abstract]

2021 Sep 15;406(2):112781. PMID: 34400174
Reprod Toxicol

GRP78 plays a key role in sperm function via the PI3K/PDK1/AKT pathway. [Abstract]

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
bioRxiv

2026 Jan 19.
bioRxiv

2025 March 11.
bioRxiv

2024 August 21.
Chemosphere

Bisphenol C induces developmental defects in liver and intestine through mTOR signaling in zebrafish (Danio rerio). [Abstract]

2023 May:322:138195. PMID: 36822516
Research Square Print

December 9th, 2022.
Dis Markers

HSPA5 Inhibitor Meliorate DSS-Induced Colitis through HSPA1A/CHIP. [Abstract]

2022 Jul 13:2022:7115181. PMID: 35872700
bioRxiv

2020 Mar.

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1433 mL

10.7163 mL

21.4326 mL

5 mM

0.4287 mL

2.1433 mL

4.2865 mL

10 mM

0.2143 mL

1.0716 mL

2.1433 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

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HA15

GSK2606414

VER-155008

BiP inducer X

Tauroursodeoxycholate

Ceapin-A7

4μ8C

YUM70

PU-WS13

4-Phenylbutyric acid

STF-083010

LY294002

HM03

Publications Citing Use of MedChemExpress (MCE) HA15

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (33)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

HA15

GSK2606414

VER-155008

BiP inducer X

Tauroursodeoxycholate

Ceapin-A7

4μ8C

YUM70

PU-WS13

4-Phenylbutyric acid

STF-083010

LY294002

HM03

Publications Citing Use of MedChemExpress (MCE) HA15

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (33)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HA15 Related Classifications

HY-100437 Related Classifications

Bioz