ttk

JAK3-IN-1 is an orally active, selective and potent JAK3 inhibitor that can be used to study immune system diseases.

CFI-402257 is a selective inhibitor of Mps1 TTK kinase (Mps1 Ki = 0.09 nM; EC50 = 6.5 nM)and can be used in studies about hepatocellular carcinoma diseases.

TTK PLK1-IN-1 (Formula I) is an inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1), with IC50 values of 7 nM and 72 nM, respectively. It regulates the spindle assembly checkpoint (SAC) and exhibits antitumor activity against triple-negative breast cancer (TNBC).

MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors. It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM. MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).

TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC 50 value of 3.0 nM.

PROTAC TTK Degrader-2 is a potent threonine tyrosine kinase (TTK) PROTAC degrader, achieving DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. It demonstrates effective target degradation and anticancer activity in a COLO-205 human colorectal cancer cell xenograft mouse model [1].

PROTAC TTK degrader-1, a potent threonine tyrosine kinase (TTK) PROTAC degrader, demonstrates DC50 values of 1.7 nM in COLO-205 cells and 5.8 nM in HCT-116 cells, indicating effective target degradation. Furthermore, it shows anticancer efficacy in a xenograft mouse model with COLO-205 human colorectal cancer cells [1].

TTK inhibitor 4 (compound 16) acts as a potent threonine tyrosine kinase (TTK) inhibitor, exhibiting an IC 50 value of 0.016 μM and demonstrating anti-tumor activity [1].

TTK21 is an activator of CBP p300 histone acetyltransferase activity.

Pal-KTTKS is a lipidated pentapeptide consisting of a fragment of the type I collagen C-terminal propeptide conjugated to palmitic acid .1 It increases collagen production in human corneal and dermal fibroblasts when used at concentrations of 0.002, 0.004, and 0.008 wt%.2 Following topical administration, pal-KTTKS (50 μg/cm2) is found in the stratum corneum, epidermis, and dermis of isolated hairless mouse skin.1 It can self-assemble into flat tapes and extended fibrillar structures.3 Pal-KTTKS has been detected in anti-wrinkle creams.4 |1. Choi, Y.L., Park, E.J., Kim, E., et al. Dermal stability and in vitro skin permeation of collagen pentapeptides (KTTKS and palmitoyl-KTTKS). Biomol. Ther. (Seoul) 22(4), 321-327 (2014).|2. Jones, R.R., Castelletto, V., Connon, C.J., et al. Collagen stimulating effect of peptide amphiphile C16-KTTKS on human fibroblasts. Mol. Pharm. 10(3), 1063-1069 (2013).|3. Castelletto, V., Hamley, I.W., Whitehouse, C., et al. Self-assembly of palmitoyl lipopeptides used in skin care products. Langmuir 29(29), 9149-9155 (2013).|4. Chirita, R.-I., Chaimbbault, P., Archambault, J.-C., et al. Development of a LC-MS/MS method to monitor palmitoyl peptides content in anti-wrinkle cosmetics. Anal. Chim. Acta 641(1-2), 95-100 (2009).

NTRC 0066-0 is an orally available, selective and potent inhibitor of threonine tyrosine kinase (TTK) that inhibits phosphorylation of TTK substrates and induces chromosome missegregation in cell lines and mice for cancer research.

CCT251455, the mitotic kinase monopolar spindle 1 (MPS1 TTK) inhibitor, is a potent (IC50=3 nM) and specific chemical tool.

PROTAC MPS1 Degrader 2 (Compound 15) is a potent degrader of monopolar spindle 1 (Mps1, TTK), AURKA, and AURKB with DC50 values of 42.0, 2.1, and 154.0 nM respectively. It is utilized in the research of acute myeloid leukemia.

PROTAC MPS1 degrader 1 (Compound 19) acts as a potent degrader of Monopolar spindle 1 (Mps1, TTK), AURKA, and AURKB, with DC50 values of 17.7, 108.7, and 570.3 nM respectively. It is utilized in the study of acute myeloid leukemia. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase)

Ro3280 (Ro5203280) is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).

CFI-401870 is an orally bioavailable potent tyrosine threonine kinase (TTK) inhibitor.

CFI-401980 is a potent and selective, novel class of TTK inhibitor.

CC-671 is a dual inhibitor of TTK protein kinase (IC50: 0.005 μM) and CLK2 (IC50: 0.006 μM).

CFI-400936 is a potent and selective TTK inhibitor with potential anticancer activity. This potent inhibitor of TTK (IC50=3.6nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases.

RMS-07, a covalent inhibitor of Monopolar Spindle Kinase 1 (MPS1 TTK), exhibits a potent inhibitory concentration (IC50) of 13.1 nM. Specifically, it targets a poorly conserved cysteine located in the hinge region of the kinase.

CFI-402257 hydrochloride, a highly selective and orally bioavailable inhibitor targeting TTK/Mps1, demonstrates an in vitro IC50 value of 1.7 nM against TTK. This compound exhibits anti-cancer activity [1].

MK2-IN-6 (Compound 11) is an effective and selective irreversible inhibitor of MK2 with an IC50 value of 2.3 nM. It suppresses the kinase activity of MK2, leading to sustained inhibition of MK2 signaling and reduction of pathological inflammatory factors in macrophages. MK2-IN-6 is capable of inhibiting the M2-like protein phenotype in macrophages both in vitro and in vivo, showing potential for use in colorectal cancer research.