Table 1 Potential small inhibitor targeting ER stress in preclinical and clinical. (ER stress, endoplasmic reticulum stress; PERK, protein kinase R-like endoplasmic reticulum kinase; IRE1α, inositol-requiring enzyme 1α; Bip, immunoglobulin binding protein.)
Molecule | Mechanism | Indication | Experimental study | Refs |
|---|---|---|---|---|
HA15 | Bip inhibitor | Osteosarcoma | In vivo | 92, 115 |
OSU-03012 | Bip inhibitor | Osteosarcoma | In vitro | 92 |
IKM5 | Bip inhibitor | Breast cancer | In vivo | 116 |
KP1339 | Bip inhibitor | Colon cancer | Phase I | 119 |
STF-083010 | IRE1α inhibitor | Multiple myeloma | In vitro | 120 |
B-I09 | Selective IRE1α RNase inhibitor | Chronic lymphocytic leukemia | In vivo | 121 |
4µ8C | IRE1α-specific inhibitor | Colon cancer | In vitro | 122 |
Compound 18 | IRE1α kinase inhibitor | Tumor | In vitro | 123–125 |
SCD1 | IRE1α RNase activity inhibitor | Burkitt’s lymphoma | In vitro | 93 |
MKC8866 | IRE1α RNase inhibitor | Glioblastoma multiforme | In vivo | 126 |
GSK2606414 | PERK inhibitor | Diabetes, neurodegenerative diseases | In vivo | 127–129 |
GSK2656157 | PERK inhibitor | Diabetes, colon cancer | In vivo | 128, 130 |
Small molecule 42,215 | PERK small molecule inhibitor | Colorectal cancer | In vitro | 131 |