TBK1

TBK1 Products

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TBK1 Inhibitors (8)
New TBK1 Products

Catalog No.	Product Name	Information	Product Use Citations
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 Vet Microbiol, 2024, 290:109973 Cell Rep, 2023, 10.1016/j.celrep.2023.113352
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 mBio, 2023, 10.1128/mbio.02506-23 Viruses, 2023, 15(5)1112
S3648	Amlexanox	Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.	Cell Commun Signal, 2024, 22(1):368 bioRxiv, 2024, 2024.09.16.613317 Signal Transduct Target Ther, 2023, 8(1):246
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.	Nature, 2024, 10.1038/s41586-024-08031-6 EMBO J, 2024, 10.1038/s44318-024-00244-9 Proc Natl Acad Sci U S A, 2024, 121(2):e2316104121
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 Vet Microbiol, 2024, 290:109973 Cell Rep, 2023, 10.1016/j.celrep.2023.113352
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 mBio, 2023, 10.1128/mbio.02506-23 Viruses, 2023, 15(5)1112
S3648	Amlexanox	Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.	Cell Commun Signal, 2024, 22(1):368 bioRxiv, 2024, 2024.09.16.613317 Signal Transduct Target Ther, 2023, 8(1):246
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.	Nature, 2024, 10.1038/s41586-024-08031-6 EMBO J, 2024, 10.1038/s44318-024-00244-9 Proc Natl Acad Sci U S A, 2024, 121(2):e2316104121
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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