Description
HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
Product information
CAS Number: 1609402-14-3
Molecular Weight: 466.58
Formula: C23H22N4O3S2
Chemical Name: N-(4-{3-[5-(dimethylamino)naphthalene-1-sulfonamido]phenyl}-1,3-thiazol-2-yl)acetamide
Smiles: CC(=O)NC1=NC(=CS1)C1=CC=CC(=C1)NS(=O)(=O)C1C=CC=C2C(=CC=CC2=1)N(C)C
InChiKey: LBSMEKVVMYSTIH-UHFFFAOYSA-N
InChi: InChI=1S/C23H22N4O3S2/c1-15(28)24-23-25-20(14-31-23)16-7-4-8-17(13-16)26-32(29,30)22-12-6-9-18-19(22)10-5-11-21(18)27(2)3/h4-14,26H,1-3H3,(H,24,25,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 50 mg/mL (107.16 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
HA15 (10 μM; 1-24 hours) induces an early endoplasmic reticulum stress (ER Stress). 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. HA15 (1-10 μM; 24 hours) induces apoptosis in A375 cells. HA15 (1-24 μM; 24 hours) induces autophagy. 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. No deleterious effects on the viability of normal human melanocytes or human fibroblasts were observed with low or high doses of HA15.
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. HA15 (0.7 mg/mouse; i.p.; 5 days/week) suppresses MPM tumor growth in vivo.
Products are for research use only. Not for human use.
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