Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response[1][2][3].
Alvespimycin hydrochloride is a potent inhibitor of Hsp90, binding to Hsp90 with EC50 of 62±29 nM.
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[1].
Apratoxin A, a cyanobacterial metabolite, mediates antiproliferative activity through the induction of G1 cell cycle arrest and an apoptotic cascade. Apratoxin A associates with Hsp70/Hsc70 to promote the degradation of Hsp90 client proteins. Apratoxin A can specifically bind the Sec61 complex[1][2][3].
Palmitic acid-1-13C is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
Palmitic acid-13C2 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
PU-H54, a Grp94-selective inhibitor, can be used for the research of breast cancer. Hsp90 chaperone family, comprised in humans of four paralogs, Hsp90α, Hsp90β, Grp94 and Trap-1, has important roles in malignancy[1].
BOLD-100 is a ruthenium-based anticancer agent. BOLD-100 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 interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution[1].
Geldanamycin is a Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria.
Palmitic acid-d17 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity[1].
ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27[1].
MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester prodrug of MPC-3100 with improved chemical stability[1].
PU-WS13 is a selective Grp94 inhibitor, with an EC50 of 0.22 μM.