HSP70 Inhibitor

HSP70 Inhibitors (37):

Cat. No.	Product Name	Effect	Purity

HY-10941

VER-155008	Inhibitor	99.82%
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.

HY-100437

HA15	Inhibitor	99.98%
HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.

HY-184106

HSP70-IN-9	Inhibitor
HSP70-IN-9 (Compound 27g) 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.

HY-10940

Pifithrin-μ	Inhibitor	99.69%
Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.

HY-15096

MKT-077	Inhibitor	98.49%
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.

HY-15098

Apoptozole	Inhibitor	99.71%
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.

HY-100110

KNK437	Inhibitor	99.04%
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.

HY-10214

SNX-2112	Inhibitor	99.49%
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.

HY-138364

YUM70	Inhibitor	98.01%
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.

HY-124611

JG-231	Inhibitor	98.47%
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.

HY-124805

MAL3-101	Inhibitor	98.22%
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).

HY-152153

GRP78-IN-3	Inhibitor	99.88%
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).

HY-162334

HYOU1-IN-1	Inhibitor	98.32%
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.

HY-12622

HSP70-IN-1	Inhibitor	98.07%
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC₅₀ of 2.3 μM.

HY-120909

YK5	Inhibitor	99.66%
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.

HY-162567

AP-4-139B	Inhibitor	98.87%
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.

HY-147039

BOLD-100 free base	Inhibitor
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.

HY-146420

GRP78-IN-2	Inhibitor
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.

HY-157085

BX-2819	Inhibitor
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.

HY-168566

EV206	Inhibitor	99.62%
EV206 is a Hsp70 binder and apoptosis inducer that binds to the N-terminal domain of Hsp70, promotes Hsp70 degradation via the ubiquitin-proteasome system, and reduces Hsp70 protein stability. EV206 induces apoptotic cell death, inhibits colony formation, and downregulates the expression of cancer stem cell-related markers in non-small cell lung cancer cells. EV206 inhibits the growth of H460 xenograft tumors in nude mice and can be used for the research of non-small cell lung cancer.

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