tbk1

H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.

CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.

Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy. MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages. MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s =250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).

TBK1 IKKε-IN-5 is a dual TBK1 and IKKε inhibitor(IC50 of 1 nM and 5.6 nM, respectively).

TBK1 IKKε-IN-1 is a dual inhibitor of TBK1 and IKKε with IC50 values of less than 100 nM.

TBK1 IKKε-IN-2 is a dual inhibitor of TBK1 and IKKε.

Negative control for TBK1 PROTAC 3i. Binds TBK1 with high affinity, but exhibits no significant degradation of TBK1. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

TBK1 IKKε-IN-4, a 6-aminopyrazolopyrimidine derivative, serves as a potent, selective inhibitor for TBK1 and IKKε, demonstrating IC50 values of 13 nM and 59 nM, respectively. This compound exhibits significantly reduced activity, by 100- to 1000-fold, against other protein kinases, such as PDK1, PI3K family members, and mTOR[1].

TBK1 IKKε-IN-6 (example 110) is a potent inhibitor of TBK1 and IKKε, exhibiting IC50 values below 100 nM for both enzymes.

TBK1-IN-1 is a specific and potent TANK-binding kinase 1 (TBK1) inhibitor (IC50: 22.4 nM) with anticancer activity.TBK1-IN-1 inhibits the expression of TBK1 downstream target genes, cxcl10 and ifnβ.

TBK1 IKKε-IN-3, a potent IP6K inhibitor, exhibits IC50 values of 3, 8.65, and 3.72 μM for IP6K1, IP6K2, and IP6K3, respectively. It is applicable in obesity disease research. [1]

TTBK1-IN-2 (N-[4-(4-chlorophenoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine) is an inhibitor of Tau-Tubulin kinase (TTBK1) with IC50s of 0.24 and 4.22 µM. TTBK1-IN-2 reduces TDP-43 phosphorylation both in cell cultures and the spinal cord of transgenic TDP-43 mice.

TTBK1-IN-1 (compound 31) is a potent and selective tau microtubule protein kinase 1 (TTBK1) inhibitor (IC50=315 nM) with central nervous system (CNS) penetration that inhibits tau phosphorylation at the disease-associated Ser 422 epitope, and can be used to study Alzheimer's disease.

(R)-TTBK1-IN-1 is a potent, selective, and brain-penetrant inhibitor of tau tubulin kinase 1 (TTBK1), acting as the enantiomer of TTBK1-IN-1, and is used in researching Alzheimer's disease and related tauopathies [1].

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

Cridanimod (10-carboxymethyl-9-acridanone, CMA) is a potent STING agonist that directly binds to STING and triggers a strong antiviral response through the TBK1 IRF3 route.

MRT199665 is an effective and ATP-competitive, selective MARK SIK AMPK inhibitor (IC50s of 2 2 3 2 nM, 10 10 nM, and 110 12 43 nM for MARK1 MARK2 MARK3 MARK14, AMPKα1 AMPKα2, and SIK1 SIK2 SIK3, respectively). MRT199665 suppresses the phosphorylation of S

MRT67307 is a kinase inhibitor of TBK1, MARK1-4, IKKε, and NUAK1 (IC50: 19, 27-52, 160, and 230 nM, respectively).

GSK8612 is a highly selective and potent inhibitor of Tank-binding Kinase-1 (TBK1, pIC50: 6.8).

Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM 6 nM 8 nM 0.5 nM and 32 nM for JAK1 JAK2 JAK3 TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

BAY-985 is a potent, selective, and orally active ATP-competitive dual inhibitor of TBK1 and IKKε (IC50s: 2 30 and 2 nM for TBK1 (low high ATP) and IKKε) with antitumor efficacy.

(Rac)-BAY-985 is a potent, ATP-competitive and selective inhibitor of TBK1(IC50 of 1.5 nM),with antitumor efficacy.

GSK319347A is a selective and potent dual inhibitor of TBK1 and IKKε with potential anti-tumor activity and inhibition of IKK2 activity, which can be used in the study of bladder cancer and lung adenocarcinoma.

BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.