tf-1

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.

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

STF-1084 is an inhibitor that cannot penetrate cells and targets ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1) with an apparent Ki of 0.11 µM. It demonstrates selectivity for ENPP1 over ENPP2 and alkaline phosphatase (ALP) with apparent Kis of 5.5 and >100 µM, respectively, and does not affect a panel of 468 kinases at 1 µM. STF-1084 hinders the extracellular breakdown of cGAMP in ENPP1-overexpressing and cGAS-expressing 293T cells, with an IC50 of 0.340 µM, and enhances mRNA expression for the gene encoding IFN-β in CD14+ primary human peripheral blood mononuclear cells (PBMCs) when incubated with conditioned medium from ENPP1-overexpressing and cGAS-expressing 293T cells treated with STF-1084. In a live setting, STF-1084, when combined with ionizing radiation, elevates the proportion of tumor-associated CD11c+ cells among antigen-presenting cells (APCs) in a murine mammary cancer model (4T1).

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

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].

SHP099 is an oral, highly selective, allosteric SHP2 (PTPN11) inhibitor with an IC₅₀ of 70 nM. SHP099 inhibits tumor cell proliferation and survival by stabilizing the autoinhibitory conformation of SHP2 and blocking RAS-ERK signaling. SHP099 inhibits the growth of cancer cells, such as MV4-11 and TF-1 cells (IC₅₀ = 0.32 and 1.73 μM). SHP099 can be used in tumor research.

Entospletinib (GS-9973) is a Syk inhibitor (IC50=7.7 nM) with selective, oral activity. Entospletinib has potential value in the treatment of a variety of hematological malignancies and immune-related diseases.

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).

Motixafortide (BKT140 4-fluorobenzoyl) is a CXCR4 antagonist with an IC50 of 1 nM.

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

Icrocaptide is used potentially for the treatment of acute myocardial infarction.

Imidazole Salicylate, a non-steroidal anti-inflammatory drug, has limited inhibitory effects on prostaglandin synthesis.

[F-18] FECNT has been widely used to calculate dopamine transporter (DAT) occupancy rates in the brains of non-human primates and can distinguish DAT density differences between Parkinson's disease and healthy human controls.

Fet F-18 is an amino acid analog radiolabeled with fluorine F-18, a positron-emitting isotope, can be used as a tracer in positron emission tomography (PET).

iCRT 14 is a novel and potent inhibitor of β-catenin-responsive transcription (CRT) with an IC50 of 40.3 nM in assays of Wnt pathway activity.

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).

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.

CP-17 is a potent and selective inhibitor of IDH2/R140Q, with an IC50 value of 40.75 nM. It demonstrates over 55-fold selectivity for wild-type IDH2. In TF-1 (IDH2/R140Q) cells, CP-17 exhibits strong D-2-HG inhibitory activity and reverses the cell differentiation block caused by the R140Q mutation. CP-17 is applicable for research in acute myeloid leukemia (AML).

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.

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.

Befovacimab (BAY 1093884) is a fully human monoclonal antibody directed against tissue factor pathway inhibitor (TFPI). By blocking the inhibitory activity of TFPI on Factor Xa and the tissue factor-Factor VIIa (TF-VIIa) complex, it restores thrombin generation, holding significant potential for the treatment research of Hemophilia A and B.

Tisotumab vedotin is an antibody-drug conjugate (ADC) targeting tissue factor (TF), consisting of the fully human monoclonal antibody (TF-011) conjugated with monomethyl auristatin E (MMAE). It exhibits significant antitumor activity and is suitable for research on the treatment of advanced or metastatic solid tumors.

Rademikibart (CBP-201) is a humanised monoclonal antibody targeting IL-4Rα (KD = 20.7 pM) that does not interact with IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signalling pathways, TF-1 cell proliferation, and TARC production in PBMCs, making it useful for studying Th2-type inflammatory diseases.

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