nih3t3

Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.

DS-1205 is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205 also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205 can inhibit cell migration in vitro and tumor growth in vivo[1].

Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

4-Methyl-2-oxopentanoic acid is an abnormal metabolite, a neurotoxin and a metabolic toxin.

Mirodenafil dihydrochloride is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Pirfenidone (AMR69) inhibits the production of CCL2 and CCL12 in fibroblasts and also decreases TGF-β2 protein levels. Pirfenidone is an antifibrotic agent that is commonly used in studies related to pulmonary fibrosis and also has anti-inflammatory activity.

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of iron death. Ferrostatin-1 potently inhibits Erastin-induced iron death in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

Vinaxanthone (SM-345431) is a small molecule compound derived from Penicillium chrysogenum that acts as a selective and potent inhibitor of semaphorin3A, phospholipase C (PLC), and FabI, exhibiting antimicrobial activity by blocking intracellular fatty acid synthesis and inhibiting the growth of Staphylococcus aureus.

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.

Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic extracted from Streptomyces kanamyceticus, which inhibits a range of Gram-positive and Gram-negative bacteria.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Afatinib (BIBW 2992) is an irreversible inhibitor of the EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M, and HER2) with IC50s of 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.

T-5224 is a transcription factor c-Fos/AP-1 inhibitor that specifically inhibits the DNA-binding activity of c-Fos/c-Jun without affecting other transcription factors.

Antibacterial agent 132 showed antimicrobial activity against C. parapsilosis (ATCC 22019) and C. krusei (ATCC 6258) with MIC90 values of <0.06 μg/mL and 62.50 μg/mL, respectively. Antibacterial agent 132 inhibited aromatase enzyme with IC50 of 0.047 μM.

Myristoyl-MEK1 Derived Peptide Inhibitor 1, the myristoylated variant of MEK1 Derived Peptide Inhibitor 1, effectively inhibits ERK activation, demonstrating an inhibitory concentration (IC50) of 10 μM [1].

J-104871 (UNII-6137X5QNJF) is a novel farnesyltransferase (FTase) inhibitor that competitively blocks Ras farnesylation in vivo, inhibits Ras processing in activated H-ras-transformed NIH3T3 cells, and suppresses tumor growth in nude mice transplanted with activated H-ras-transformed NIH3T3 cells.

A-176120 is a potent farnesyl pyrophosphate (FPP) analogues, it selectively inhibits farnesyltransferase. It has anti-angiogenic potential and may reduce H-ras NIH3T3 tumour growth.

CEP-751 (also known as KT-6587) is a potent Trk inhibitor. It exhibits significant growth inhibition in MBL cell line D283 (Day 39, P=0.031) and demonstrates moderate growth inhibition in IMR5 (P=0.062) and CHP-134 (P=0.049) cell lines. Additionally, CEP-751 induces apoptosis in CHP-134 tumors. It may be a useful compound for treating NBL or MBL. At a concentration of 100 nM, CEP-751 inhibits the receptor tyrosine kinase activity of neurotrophin receptors trkA, trkB, and trkC. It also shows antitumor effects on tumors derived from trkA-transfected NIH3T3 cells.

Topoisomerase I inhibitor 14 (Compound 4h) acts as an inhibitor of topoisomerase I. It suppresses the proliferation of A549 and C6 cells, with IC50 values of 4.56 μM and 13.17 μM, respectively. The compound shows no significant toxicity towards healthy NIH3T3 cells (IC50 of 74.44 μM) and demonstrates anticancer activity.

α-hydroxy Farnesyl phosphonic acid, a nonhydrolyzable analog of farnesyl pyrophosphate, acts as a competitive inhibitor of farnesyl transferase (FTase). At concentrations above 1 μM, it inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells.

GGTI-286 is a potent, cell permeable GGTase I inhibitor (IC50: 2 μM). GGTI-286 inhibits Rap1A geranylation in NIH3T3 cells (IC50: 2 μM) more potently than H-Ras farnesylation (IC50>30 μM). Ras4B stimulation (IC50: 1 μM).

TGFβRI-IN-4 is a potent, orally active TGFβ receptor type I kinase (TGFβRI) inhibitor that targets ALK5 (IC50: 44 nM) and NIH3T3 (IC50: 42.5 nM), inhibiting tumor growth and weight in a xenograft tumor model.