tafi

IQB-782 is a mucolytic agent with mucolytic expectorant activity.IQB-782 inhibits thrombin-activating fibrinolytic inhibitor (TAFI), protects rats from tobacco smoke-induced respiratory obstruction, reduces the viscosity of gastric mucin suspensions in vitro, and may be useful in studies of obstructive lung disease.IQB-782 has been shown to reduce the viscosity of gastric mucin suspensions in vitro.

Razuprotafib (AKB-9778) is a protein tyrosine phosphatase ß (HPTPß) inhibitor with an IC50 of 50 nM. It effectively activates Tie-2 and provides protection against acute kidney injury.

Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.

Dasantafil (SCH446132) is a small molecule phosphodiesterase-5A (PDE5A) inhibitor used to treat genitourinary disorders and study erectile dysfunction.

Stafib-2 is a potent and selective inhibitor of the transcription factor STAT5b, with IC50 values of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively. Stafib-2 has poor cell permeability.

Osunprotafib (ABBV-CLS-484) hydrochloride is an orally active, selective inhibitor targeting the active sites of PTPN1 (IC50: 2.5 nM) and PTPN2 (IC50: 1.8 nM). It shows 6-8 times weaker activity towards PTPN9 and no detectable activity against SHP-1 or SHP-2. This compound enhances the sensitivity of human cancer cell lines to IFNγ. By boosting JAK-STAT signaling and reducing T cell dysfunction, Osunprotafib hydrochloride exhibits potent antitumor immunity.

Razuprotafib (AKB-9778) sodium is a potent and selective inhibitor of VE-PTP (HPTPη) catalytic activity, with an IC50 of 17 pM. It promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib sodium also inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Additionally, apart from HPTPη (IC50 of 36 pM) and HPTPγ (100 pM), it has good selectivity for VE-PTP.

Stafib-1 is a selective inhibitor of STAT5β targeting SH2 domain with an IC50 of 154 nM and a Ki of 44 nM.

Stafia-1-dipivaloyloxymethyl ester (compound 27) demonstrated a dose-dependent reduction in pSTAT5a expression (0-200 μM) while showing no discernible effect on pSTAT5b[1].

Migoprotafib (GDC-1971) is a potent and highly selective SHP2 (Src Homology-2 Domain-Containing Phosphatase 2) inhibitor for the study of advanced solid tumours.

PomCapstafin is a prodrug of Capstafin, acting as a potent, selective STAT5b inhibitor.

Capstafin is a highly potent and selective inhibitor of STAT5b.

Pomstafib-2, a potent and selective inhibitor of STAT5b, reduces pSTAT5b expression and effectively induces apoptosis [1] [2].

Tegeprotafib (PTPN2/1-IN-1) is an orally active and potent PTPN1/2 inhibitor with potential anticancer and antitumor activity for the study of cancer and immune system diseases.

Stafia-1 is a potent STAT5a inhibitor (IC50=22.2 μM), displaying high selectivity over STAT5b and other STAT family members.

DS-1040 Tosylate is a thrombin-activated fibrinolysis inhibitor (TAFIa) inhibitor, also a fibrinolysis enhancer, inhibiting TAFIa and carboxypeptidase N, reducing fibrin clots in the lungs, useful in thromboembolic disease research.

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

CDK8-IN-4k is a potent and highly selective CDK8 inhibitor, with no apparent potential for time-dependent CYP3A4 inhibition.

UK-396082 is a thrombin-activated fibrinolysis inhibitor (TAFI) that inhibits Carboxypeptidase B. It is used in the study of thrombosis, atherosclerosis, cancer, and fibrotic conditions.

Glycylglycylcysteine is an inhibitor of Thrombin Activatable Fibrinolysis Inhibitor (TAFI), exhibiting a K_i value of 0.99 µM and an IC_50 of 9.4 µM in TAFI substrate assays. TAFI, a basic carboxypeptidase, hinders fibrinolysis by cleaving C-terminal lysine residues on partially degraded fibrin [1].