ttbk1 in 1

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.

TTBK1/2-IN-3 (compound 10) is a potent inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 579 nM and 258 nM, respectively. TTBK1/2-IN-3 can reduce the expression of primary cilia on the surface of human induced pluripotent stem cells (iPSC).

TTBK1/2-IN-1 (compound 3) is a potent inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 816 nM and 384 nM, respectively.

TTBK1/2-IN-2 (compound 9) is a potent inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 384 nM and 175 nM, respectively. In human induced pluripotent stem cells (iPSC), TTBK1/2-IN-2 demonstrates a significant ciliogenesis phenotype.

(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].