S8299 |
HA15 |
HA15 is a molecule that targets specifically HSPA5 (Heat shock 70kDa protein 5) also known as BiP (Immunoglobulin heavy-chain-binding protein) or Grp78 (glucose-regulated protein 78). HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors. |
Selective |
|
S8365 |
Apoptozole |
Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis. |
Selective |
HSP70, Kd: 0.14 μM; HSC70, Kd: 0.21 μM |
S7751 |
VER155008 |
VER155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins. |
Selective |
HSP70, IC50: 0.5 μM; HSC70, IC50: 2.6 μM; GRP78, IC50: 2.6 μM |
S6193 |
YUM70 |
YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.Although YUM70 inhibits GRP78 enzymatic activity, it increases the expression of GRP78 by increasing the chaperone translation mechanism. |
Selective |
GRP78, IC50: 1.5 μM |
S6721 |
JG98 |
JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. JG-98 induces classical apoptosis features, including morphological changes consistent with programmed cell death and positive annexin staining. JG-98 exhibits anticancer activity. |
Selective |
|
S1052 |
Elesclomol (STA-4783) |
Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand and inhibits FDX1-mediated Fe-S cluster biosynthesis.Elesclomol (STA-4783) is a potent copper ionophore and can be used in the research of copper-dependent cell death (cuproptosis). |
Selective |
|
S8305 |
TRC051384 |
TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent. |
Selective |
|
S6568 |
ML346 |
ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases. |
Selective |
|
S7750 |
KNK437 |
KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
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Pan |
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