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HA15 HSP modulator

Cat.No.S8299

HA15 is a molecule that targets specifically HSPA5 (Heat shock 70kDa protein 5) also known as BiP (Immunoglobulin heavy-chain-binding protein) or Grp78 (glucose-regulated protein 78). This compound displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.
HA15 HSP modulator Chemical Structure

Chemical Structure

Molecular Weight: 466.58

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Quality Control

Batch: S829901 DMSO]93 mg/mL]false]Ethanol]45 mg/mL]false]Water]Insoluble]false Purity: 99.64%
99.64

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (199.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 45 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 466.58 Formula

C23H22N4O3S2

Storage (From the date of receipt)
CAS No. 1609402-14-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(=O)NC1=NC(=CS1)C2=CC(=CC=C2)NS(=O)(=O)C3=CC=CC4=C3C=CC=C4N(C)C

Mechanism of Action

Targets/IC50/Ki
BiP/GRP78/HSPA5
In vitro
HA15 induces ER stress leading to cancer cell death in vitro and overcomes BRAF inhibitor resistance in melanoma cells.
In vivo
HA15 induces ER stress leading to cancer cell death and exhibits strong efficacy in xenograft mouse models with melanoma cells either sensitive or resistant to BRAF inhibitors.
References

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