| DC10037 |
4μ8C
Featured
|
4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM. |
|
| DC7358 |
APY29
Featured
|
APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity. |
|
| DC10544 |
MKC3946
Featured
|
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research. |
|
| DC8413 |
STF-083010
Featured
|
STF-083010 is a specific IRE1α endonuclease inhibitor. |
|
| DC48263 |
IRE1α kinase-IN-6 |
IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM. |
|
| DC70125 |
GSK2850163 |
A novel potent IRE1α-selective kinase inhibitor that inhibits both the kinase and RNase activities of IRE1α with IC50 of 20 nM and 200 nM, respectively; binds to pIRE1α and inhibits XBP 1 splicing; only weakly inhibits Ron (IC50= 4.4 uM) and FGFR1 V561M (IC50=17 uM) in a panel of 284 kinases. |
|
| DC71145 |
KIRA9 |
KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis. |
|
| DC71403 |
PAIR2 |
PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing. |
|
| DC73837 |
D-F07 |
D-F07 is a novel fluorescent, covalent IRE-1 inhibitor, potently inhibits XBP-1s expression in MM cells. |
|
| DC73838 |
PAIR1 |
PAIR1 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=220 nM) but only partially inhibit its RNase activity. |
|
| DC73839 |
TC-D-F07 |
TC-D-F07 is a novel prodrug of the covalent IRE-1 inhibitor D-F07, inhibits IRE-1/XBP-1s pathway in cancer cells. |
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