tg-2

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.

ZED-1227 (TAK-227) is an orally active, selective and potent transglutaminase 2 (TG2) inhibitor with anticancer activity that blocks inflammation-induced TG2 expression and activation for the treatment of Celiac Disease.

TG2-IN-3h is a transglutaminase (TGase) inhibitor used in the study of neurological and immune system disorders.

AA10 is an irreversible inhibitor of transglutaminase 2 (TG2).

VA5 is an transamidase inhibitor by direct binding at the transamidase site. VA5 also inhibits GTP-binding activities. It interaction at the transamidase site locks the protein in the extended/open conformation to disorganize/inactivate the GTP binding/GT

AA9 is a novel transglutaminase (TG2) inhibitor.

VA4 is a novel irreversible TG2 transamidase site-specific inhibitor.

PNU-145156E (formerly FCE 26644) is a noncytotoxic small molecule that exerts antitumor activity through reversible complex formation with growth and angiogenic factors, thereby inhibiting their ability to induce angiogenesis. PNU-145156E is utilized in research on tumor vascularization, angiogenesis regulation, and the development of anti-angiogenic therapeutic strategies.

PROTAC TG2 degrader-2 (compound 7) is a selective competitive degrader of Transglutaminase 2 (TG2) with a dissociation constant (Kd) greater than 100 μM. It inhibits cell migration and reduces TG2 levels in ovarian cancer cells, making it a valuable tool for ovarian cancer research [1].

PROTAC TG2 Degrader-1 (Compound 11) is a VHL-based PROTAC that targets tissue transglutaminase (TG2) and exhibits a binding affinity with a K D of 68.9 μM. This compound effectively decreases TG2 levels in ovarian cancer cells through a proteasome-dependent pathway [1].

TG-2-IN-4 (compound 8), an inhibitor of transglutaminase 2 (TG2) with an IC 50 value of less than 0.5 mM, is utilized in the study of inflammatory disorders [1].

NC9 is an irreversible inhibitor of transglutaminase 2 (TG2) and also inhibits Factor XIIIA (FXIIIA).

BJJF078, an aminopiperidine derivative, is a potent inhibitor of recombinant human and mouse glutamine aminotransferase (TG2) activity, with IC50 values of 41 and 54 nM for human and mouse glutamine aminotransferase, respectively.BJJF078 inhibits TG1 enzyme, with an IC50 of 0.16 μM.BJJF078 can be used to study multiple sclerosis (MS). BJJF078 can be used to study multiple sclerosis (MS).

TG2-179-1 is a BRCA1-associated protein 1 (BAP1) inhibitor with potential anticancer activity. TG2-179-1 exhibits potent cytotoxic activity against colon cancer cells and induces apoptosis. TG2-179-1 can be used in colon cancer research. TG2-179-1 is a BRCA1-associated protein 1 (BAP1) inhibitor with potential anticancer activity.

NVS-STG2 is a STING agonist that promotes the oligomerization of human STING by binding to the pockets between adjacent STING dimer transmembrane domains, effectively acting as molecular glue. It triggers strong STING-mediated immune responses in cells and demonstrates antitumor activity in hSTING knock-in mice.

ppTG20 is an amphiphilic cell-penetrating peptide (KALA) utilized for gene transfection. It has the ability to bind with DNA, disrupt membrane stability, and mediate DNA transfection.

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).

6-Thioguanine (2-Amino-6-purinethiol) is an antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.

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,

TKB272 is an orally active antiviral agent that selectively targets the main protease (Mpro) of SARS-CoV-2, effectively inhibiting the infection and replication of various strains, including Omicron variants (such as XBB.1.5 and EG.5.1). It exhibits an enzyme inhibitory activity with an IC50 of 0.7 µM against SARS-CoV-2WK-521 Mpro and shows potent antiviral activity at the cellular level with an EC50 as low as 2.6 nM in HeLahACE2-TMPRSS2 cells against the BQ.1.1 strain. TKB272 also has a CC50 of 98 µM, indicating low cytotoxicity. Furthermore, it demonstrates a significant suppression of SARS-CoV-2XBB.1.5 replication in the B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse model, suggesting potential use in the research of SARS-CoV-2 infections.

JTT-553 is a DGAT1 inhibitor with an IC50 of 2.38 nM. It effectively reduces plasma levels of glucose, insulin, non-esterified fatty acids (NEFA), total cholesterol (TC), and liver triglycerides (TG). JTT-553 enhances insulin-dependent glucose absorption and glucose intolerance in the adipose tissue of diet-induced obese (DIO) mice. In KK-Ay mice, it lowers TNF-α mRNA levels and elevates GLUT4 mRNA levels in adipose tissue. By contributing to weight loss, JTT-553 improves insulin resistance in adipose tissue and overall glucose metabolism. This compound is useful for research on obesity and type 2 diabetes mellitus (T2DM).

1-Palmitoyl-2-10-pahsa-3-oleoyl-sn-glycerol (16:0-10-Pahsa-18:1-TG) is a triglyceride composed of fatty acid esters including Palmitic acid, hydroxy fatty acid (FAHFA) 10-PAHSA, and Oleic acid.

Salvifaricin, an orally active diterpenoid isolated from Salvia leucantha Cav. and Salvia hispanica L., significantly lowers fasting blood glucose and serum triglyceride (TG) levels, exhibiting an anti-diabetic effect [1] [2].