tf-1

NVS-BPTF-1 is a specific inhibitor of bromodomain and PHD finger containing transcription factor (BPTF), exhibiting a dissociation constant (K_D) of 71 nM [1].

STF-118804, a highly specific NAMPT inhibitor, reduces the viability of most B-ALL cell lines with an IC50 of less than 10 nM.

IDH2R140Q-IN-2 is an orally active and potent IDH2R140Q inhibitor with an IC50 of 29 nM.IDH2R140Q-IN-2 possesses potential antitumour activity, reducing D2HG production in TF-1 cell lines carrying the IDH2R140Q mutation (IC50 of 10 nM) and inhibiting tumour tissue D2HG levels.IDH2R140Q-IN-2 is suitable for the study of acute myeloid leukaemia (AML).

Cefazolin is a semi-synthetic cephalosporin that has a broad spectrum of antibacterial activity and inhibits the synthesis of bacterial cell walls.

Cefazolin sodium (cephazolin sodium) salt binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Cefazolin sodium salt is the sodium salt of cefazolin, a beta-lactam antibiotic and first-generation cephalosporin with bactericidal activity. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, which results in the weakening of the bacterial cell wall and cell lysis.

SHP099 (SHP099 free base) free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models.

Entospletinib (GS-9973) (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable.

Talacotuzumab (JNJ 56022473) is an IgG1 fully humanized CD123 neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has a high affinity for CD123, CD32b c, CD16-158F and CD16-158V, with KD of 0.43 nM, 188 nM, 46 nM and 16.8 nM, respectively. Talacotuzumab inhibits IL-3 signaling in target cells by inhibiting IL-3 binding to CD123. Talacotuzumab induces mutations in the Fc region to increase affinity for CD16 (FCγriiia), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab inhibits leukemia cell growth in xenografted mouse models of acute myeloid leukemia (AML).

Anpocogin, a variant of the Ancyclostoma canium nematode anticoagulant protein c2 with an added C-terminal P85, is synthesized in Pichia pastoris and functions as an anticoagulant agent [1].Recombinant nematode anticoagulant protein c2 (rNAPc2) is a potent inhibitor of serine protease factor VIIa and its cell-associated cofactor tissue factor FVIIa TF, a key physiological initiator of blood coagulation, with potential efficacy in the treatment of disseminated intravascular coagulopathy and venous and arterial thrombosis.

Rademikibart (CBP-201) is a human monoclonal antibody selective for IL-4Rα, exhibiting strong affinity with a KD of 20.7 pM for human IL-4Rα epitopes, without cross-reactivity to IL-4Rα from other species. It effectively inhibits IL-4 and IL-13-induced STAT6 signaling, TF-1 cell proliferation, and TARC production in PBMCs, showing promise for investigating moderate-to-severe Th2 inflammatory diseases [1].

1. Ruscogenin has anti-inflammatory activity, suppressed zymosan A-evoked peritoneal total leukocyte migration in mice in a dose-dependent manner, 2. Ruscogenin inhibited adhesion of leukocytes to a human umbilical vein endothelial cell line (ECV34) injured by tumor necrosis factor-alpha (TNF-alpha) in a concentration-dependent manner. 3. Ruscogenin significantly attenuate LPS-induced acute lung injury via inhibiting expressions of TF and iNOS and NF-kappa B p65 activation.

Tisotumab vedotin is an antibody-drug conjugate (ADC) that targets tissue factor (TF), combining a fully human monoclonal antibody against TF (TF-011) with the cytotoxic agent Monomethyl Auristatin E (MMAE), and exhibits potent antitumor activity in advanced or metastatic solid tumors [1].

Transferrin aldifitox (TF-CRM107), a conjugate of diphtheria toxin CRM107 with transferrin, can be used for anticancer research [1].

JAK-IN-39 (compound 11) is a JAK inhibitor with IC50 values of 0.05 nM for JAK1, 1.18 nM for JAK2, and 0.03 nM for JAK3. It reduces cell viability in TF-1 cells and inhibits the production of TNFα and INFγ in lymphocytes in vitro.