TBK1

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Catalog No. Product Name Information Product Use Citations Product Validations
S1274 BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.
Vet Microbiol, 2024, 290:109973
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
Cell Rep, 2023, 42(2):112127
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
Cancer Res, 2022, 82(10):1991-2002
S3648 Amlexanox Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
Signal Transduct Target Ther, 2023, 8(1):246
Signal Transduct Target Ther, 2023, 8(1):246
Nucleic Acids Res, 2022, 50(15):8700-8718
S8872 GSK8612 GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified.
Proc Natl Acad Sci U S A, 2024, 121(2):e2316104121
Int J Biol Sci, 2023, 19(3):981-993
Int J Biol Sci, 2023, 19(3):981-993
S8922 TBK1/IKKε-IN-5 TBK1/IKKε-IN-5 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo.
Sci Adv, 2024, 10(6):eadk2285
Cell Rep, 2023, 42(2):112127
J Nat Prod, 2023, acs.jnatprod.2c00843
S8935 BAY-985 BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM).
Nat Commun, 2023, 14(1):1399
Nat Commun, 2023, 14(1):1399
Mol Cancer, 2022, 21(1):97
S6386 MRT67307

MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells.

Front Pharmacol, 2022, 13:924523
Microbiol Spectr, 2022, e0219321
S0425 TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε.
Int J Mol Sci, 2022, 23(23)15000
S1274 BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.
Vet Microbiol, 2024, 290:109973
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
Cell Rep, 2023, 42(2):112127
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
Cancer Res, 2022, 82(10):1991-2002
S3648 Amlexanox Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
Signal Transduct Target Ther, 2023, 8(1):246
Signal Transduct Target Ther, 2023, 8(1):246
Nucleic Acids Res, 2022, 50(15):8700-8718
S8872 GSK8612 GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified.
Proc Natl Acad Sci U S A, 2024, 121(2):e2316104121
Int J Biol Sci, 2023, 19(3):981-993
Int J Biol Sci, 2023, 19(3):981-993
S8922 TBK1/IKKε-IN-5 TBK1/IKKε-IN-5 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo.
Sci Adv, 2024, 10(6):eadk2285
Cell Rep, 2023, 42(2):112127
J Nat Prod, 2023, acs.jnatprod.2c00843
S8935 BAY-985 BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM).
Nat Commun, 2023, 14(1):1399
Nat Commun, 2023, 14(1):1399
Mol Cancer, 2022, 21(1):97
S6386 MRT67307

MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells.

Front Pharmacol, 2022, 13:924523
Microbiol Spectr, 2022, e0219321
S0425 TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε.
Int J Mol Sci, 2022, 23(23)15000

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