KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
KI696 细胞实验
Cell Line
Concentration
Treated Time
Description
References
KP cells
1 µM
36 hr
To validate that treatment with KI696 could increase Nrf2 protein levels as well as increase expression of downstream target genes in KP cells, and induce sensitivity to CB-839.
Elife. 2017 Oct 2;6:e28083.
H2009 cells
1 µM
36 hr
To validate that treatment with KI696 could increase NRF2 protein levels as well as increase expression of downstream target genes in H2009 cells, and induce sensitivity to CB-839.
Elife. 2017 Oct 2;6:e28083.
KP cells
1 μM
96 h
To evaluate the effect of KI696 on the sensitivity of KP cells to PARP inhibitors
Cell. 2022 Jan 6;185(1):169-183.e19.
non-small cell lung cancer cell lines
1 μM
48 h
To investigate the effect of KI696 on the proliferation of non-small cell lung cancer cell lines, it was found that KI696 significantly inhibited proliferation in some cell lines
Cell Metab. 2023 Mar 7;35(3):487-503.e7.
HEK293T cells
5 μM
24 h
KI696 treatment restored DPP9 activity, indicating that KEAP1 binding was responsible for DPP9 inhibition.
To evaluate the growth inhibitory effect of KI696 on cells under serine or asparagine deprivation, results showed that KI696 treatment significantly inhibited cell growth.
To evaluate the growth inhibitory effect of KI696 on cells under serine or asparagine deprivation, results showed that KI696 treatment significantly inhibited cell growth.
Cell Metab. 2020 Feb 4;31(2):339-350.e4.
mouse KrasG12D/+; p53−/− pancreatic cancer cells
1μM
3 days
To evaluate the growth inhibitory effect of KI696 on cells under serine deprivation, results showed that KI696 treatment significantly inhibited cell growth.
Cell Metab. 2020 Feb 4;31(2):339-350.e4.
non-small cell lung cancer cell lines
1 μM
48 h
To evaluate the effect of KI696 on cell proliferation, it was found that more than 13% of the cell lines showed significant inhibition of proliferation after KI696 treatment
Cell Metab. 2023 Mar 7;35(3):487-503.e7.
KI696 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
C57BL/6J mice
Intraperitoneal injection
0.66 mg/kg
Once a day for 15 days
To evaluate the therapeutic effect of PARP inhibitors on KEAP1-mutant tumors
Cell. 2022 Jan 6;185(1):169-183.e19.
Mice
Patient-derived xenograft model (PDX)
Oral gavage
5 mg/kg
3 times a week for 3 weeks
To investigate the inhibitory effect of IACS-010759 on KEAP1-mutant tumors, it was found that IACS-010759 significantly inhibited the growth of KEAP1-mutant tumors
Cell Metab. 2023 Mar 7;35(3):487-503.e7.
Mice
Patient-derived xenograft (PDX) model
Oral
5 mg/kg
3 times a week for a total of 3 weeks
To evaluate the growth inhibitory effect of IACS-010759 on KEAP1-mutant tumors, it was found that IACS-010759 significantly inhibited the growth of KEAP1-mutant tumors
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