An inhibitor of GRP78
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HA-15

Item No. 35775

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[3-[[[5-(dimethylamino)-1-naphthalenyl]sulfonyl]amino]phenyl]-2-thiazolyl]-acetamide
CAS Number
1609402-14-3
Molecular Formula
C23H22N4O3S2
Formula Weight
466.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 30 mg/mlEthanol: 15 mg/mlPBS (pH 7.2): insol
λmax
219 nm
SMILES
O=C(C)NC1=NC(C2=CC(NS(=O)(C3=CC=CC4=C(N(C)C)C=CC=C43)=O)=CC=C2)=CS1
InChi Code
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)
InChi Key
LBSMEKVVMYSTIH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Cayman Chemical
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    Product Description

    HA-15 is an inhibitor of glucose-regulated protein 78 kDa (GRP78), also known as heat shock 70 kDa protein 5 (HspA5) and immunoglobulin heavy chain-binding protein (BiP), a cellular chaperone.1 It binds to GRP79 in a cell-free assay and increases the expression of the genes encoding the unfolded protein response (UPR) proteins EIF2AK3, IRE1α, ATF6, DDIT3, and XBP1, as well as the apoptosis-associated genes JUN and BCL2 and the autophagy marker gene LC3. HA-15 decreases the viability of A375 melanoma cells (IC50 = 2.5 µM). In vivo, HA-15 (0.7 mg/animal per day) reduces tumor volume and induces intratumor apoptosis and autophagy in an A375 mouse xenograft model. HA-15 also increases osteogenesis and reduces bone loss in a mouse model of ovariectomy-induced osteoporosis.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cerezo, M., Lehraiki, A., Millet, A., et al. Compounds triggering ER stress exert anti-melanoma effects and overcome BRAF inhibitor resistance. Cancer Cell 29(6), 805-819 (2016).

    2. Han, C., Xie, K., Yang, C., et al. HA15 alleviates bone loss in ovariectomy-induced osteoporosis by targeting HSPA5. Exp. Cell Res. 406(2), 112781 (2021).