tg

Transglutaminase (TG) is a thiolase that induces intermolecular cross-linking of proteins, by catalysing the formation of isopeptide bonds between the γ-carboxamide group of glutamine residues and the primary ε-amine group of other compounds. The enzyme plays a role in a variety of physiological processes including coagulation, antimicrobial immune responses and photosynthesis.

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).

TG-89 is an inhibitor of JAK2, JAK3, RET and FLT3, and has an IC50 value of 11.2 μM against JAK2, showing anticancer activity in the treatment of ovarian and cervical cancer.

TG-46 (TG46) inhibits JAK2, FLT3, RET, JAK3 and can be used to study glaucoma.

TG 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

TG 100801 Hydrochloride is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src,

(E/Z)-TG003 is a potent and ATP-competitive inhibitor of Cdc2-like kinase (Clk).

TG-100435 is a novel multi-target oral protein tyrosine kinase inhibitor. The metabolic flux of TG100435 is entirely inhibited by methimazole and ketoconazole. In human liver microsomes or recombinant P450, the formation of TG100435 increases with the activity of cytochrome P450 reductase, suggesting that cytochrome P450 reductase may be involved.

TG6-10-1 is an EP2 antagonist.

TG41 is a GABAA receptors positive modulator.

TG53 is a tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction inhibitor.

TG100-115 is a PI3Kγ/δ inhibitor (IC50: 83/235 nM), with fewer effects on PI3Kα/β.

TG6-129 is an antagonist of the EP2 receptor. TG6-129 suppresses PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM. TG6-129 reduces the expression of COX-2, IL-1β, IL-6, IL-12, IL-23 and TNF-α induced by the EP2-selective

TG101209 is a selective JAK2 inhibitor with an IC50 of 6 nM.

TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels

TG-2-IN-1 is a potent transglutaminase-2 (TGM-2) inhibitor.TG-2-IN-1 is used in the study of cancer, neurological disorders, and immune system disorders.

TG003 is a potent Clk1/Sty inhibitor that inhibits Clk1 and Clk4, inhibits cancer cell growth and induces apoptosis, and can be used in the study of Duchenne muscular dystrophy.

TG-693 is an orally active CLK1 (CDC2-like kinase 1) inhibitor that promotes exon 31 skipping of the dystrophin gene mutation in vivo and inhibits CLK1 substrate phosphorylation, suitable for studying Duchenne muscular dystrophy (DMD).

TG 100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.

TG11-77 HCl is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 HCl has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 HCl are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties.

TG11-77 free base is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 free base has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 free base are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties.

TG100948 is a novel dual VEGFR/Src kinase inhibitor.

HAT-SIL-TG-1&AT, a hypoxia-activated prodrug, functions as a Janus tyrosine kinase (JAK) inhibitor demonstrating antitumor effects by inhibiting JAK-STAT signaling within tumor tissues. It also suppresses the proliferation of HEL cells and downregulates phosphorylated STAT3/5 in hypoxic conditions.