HSP70 Inhibitor

VER-155008 is an inhibitor of Hsp70, with IC₅₀s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a K_d of 0.3 μM for Hsp70.

HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.

HSP70-IN-9 is a Hsp70 inhibitor. HSP70-IN-9 activates Caspase-3 and -7. HSP70-IN-9 exerts anticancer effects against acute myeloid leukemia. HSP70-IN-9 can be used for the research of acute myeloid leukemia.

Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.

MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity. MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm.

Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with K_ds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.

KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.

SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a K_d of 16 nM for Hsp90 and IC₅₀s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC₅₀s of 10 nM, 4.275 μM and 0.862 μM, respectively. SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with K_ds of 4 nM, 6 nM and 484 nM, respectively.

YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC₅₀ of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model.

JG-231 is an allosteric inhibitor of heat shock protein 70 (Hsp70). JG - 231 inhibits the binding of Hsp70 and BAG family proteins, including inhibition of Hsp70 and BAG1 with a K_i of 0.11 μM. JG-231 inhibits proliferation of tumor cells and induces apoptosis. JG-231 has antitumor activity.

MAL3-101 is a potent HSP70 allosteric inhibitor. MAL3-101 inhibits HSP70 ATPase activity by blocking Hsp40 co-chaperone interaction. MAL3-101 can be used for researching muscle invasive bladder cancer (MIBC).

GRP78-IN-3 (Compound 8) is a selective Grp78 (HSPA5) inhibitor with an IC₅₀ of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC₅₀ of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC₅₀ of 13.9 μM).

HYOU1-IN-1 (Compound 33) is an inhibitor of hypoxia-upregulated protein 1 (HYOU1) with anti-inflammatory activity. HYOU1-IN-1 can be used in research on the regulation of fibroblast activation, chronic inflammation, and fibrotic diseases.

HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC₅₀ of 2.3 μM.

YK5 is a potent and selective Hsp70 inhibitor. YK5 selectively and tightly binds to the cytosolic Hsp70s in cancer cells. YK5 has biological activity partly by interfering with the formation of active oncogenic Hsp70/Hsp90/client protein complexes.

AP-4-139B is a blood-brain barrier-permeable HSP70 inhibitor with a IC₅₀ of 180 nM against hHSP70. AP-4-139B binds directly to HSP70 and inhibits its ATPase activity. AP-4-139B promotes Autophagy by increasing the phosphorylation of Beclin-1. AP-4-139B exerts antitumor effects in preclinical models of colorectal cancer and pancreatic ductal adenocarcinoma.

Zinc picolinate is an orally effective zinc supplement. Zinc picolinate reduces the expression of Hsp70, inhibits oxidative DNA damage, increases serum ALP activity, decreases MDA concentration, elevates SOD levels, and raises zinc concentrations in serum, whole body and plasma. Zinc picolinate does not alter copper and manganese contents in rainbow trout. Zinc picolinate exerts a protective effect against Acetic acid (HY-Y0319)-induced experimental colitis in Sprague Dawley rats. Zinc picolinate reduces uterine fibroid volume, alleviates colonic oxidative damage, relieves colonic inflammation, and enhances intestinal barrier integrity. Zinc picolinate can be used in research related to uterine fibroids, ulcerative colitis and chronic obstructive pulmonary disease.

BOLD-100 (NKP-1339; IT-139) free base is a ruthenium-based anticancer agent. BOLD-100 free base also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 free base interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution.

GRP78-IN-2 (Compound FL5) is a GRP78 (Glucose Regulated Protein 78 kDa) inhibitor. GRP78-IN-2 preferentially targeting cell surface GRP78 and shows potent antiangiogenic and anticancer activities without affecting other normal cells.

BX-2819 is a Hsp90 inhibitor with an IC₅₀ value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice.