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

HA15 

Cat. No.: HY-100437 Purity: 99.84%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
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10 mg USD 132 In-stock
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50 mg USD 420 In-stock
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100 mg USD 720 In-stock
Estimated Time of Arrival: December 31
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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].

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].

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.
Molecular Weight

466.58

Formula

C₂₃H₂₂N₄O₃S₂

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (107.16 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
10 mM 0.2143 mL 1.0716 mL 2.1433 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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