b16-f10

FAK-IN-7 has potential antiproliferative activity and is a FAK inhibitor.

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory and immunosuppressive properties that induces autophagy and inhibits LPS-induced inflammatory responses in macrophages.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1 2 3 6 7 11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

Tamoxifen (ICI47699) is a selective and orally effective estrogen receptor modulator (SERM). Tamoxifen has both inhibitory (e.g., mammary cells) and activating (e.g., bone, liver, and uterine cells) activity against estrogens.

FR-167356 is a specific inhibitor of a3 isoform vacuolar type H⁺-ATPase with IC50s of 170 nM, 370 nM and 220 nM for osteoclast plasma membranes, renal brush border membranes and macrophage microsomes. FR-167356 reduces bone metastasis of B16-F10 cells.

Ursolic acid (Prunol) is a natural product, a pentacyclic triterpene carboxylic acid extracted from Rhododendron caprifolium. Ursolic acid has anti-tumor, anti-inflammatory, anti-bacterial and hypoglycemic activities.

Ribociclib (LEE011) is an orally available, and highly specific CDK4 6 inhibitor (IC50:10 39 nM).

Calcitriol (1,25-Dihydroxyvitamin D3) is a metabolite of vitamin D and a vitamin D receptor (VDR) agonist (IC50=0.4 nM). Calcitriol increases intestinal absorption of calcium and phosphorus, and increases bone resorption with parathyroid hormone.

ALPHA-PINENE ((-)-Alpha-Pinene) is a bicyclic monoterpene found in pine trees and other plants, including Cannabis with diverse biological activities [1]. It reduces the growth of a panel of seven Gram-positive bacteria, seven Gram-negative bacteria, and eight yeast strains with MIC values of 0.75-1.29, 1.05-1.59, and 0.7-1.17%, respectively [2]. It has insecticidal activity against C. molestus larvae with LC50 values ranging from 47 to 49 mg L.3 ALPHA-PINENE (100 μg ml) induces apoptosis, increases anion superoxide production and DNA fragmentation, and activates caspase-3 in B16 F10 melanoma cells [4]. In a B16 F10 mouse xenograft model, ALPHA-PINENE(100 ml of a 10 mg ml solution) reduces the number of metastatic lung nodules by approximately 7-fold. ALPHA-PINENE(8.6 mg L, aerosol) also increases the time spent in the open arms of the elevated plus maze by approximately 2-fold in mice, indicating anxiolytic-like activity [5].

Antitumor Agent-184 (compound 12aa) triggers apoptosis in various cell lines, exhibiting IC50 values of 2.35 μM in B16-F10 cells, 7.32 μM in 4T1 cells, and 10.31 μM in CT26 cells.

IDO1 TDO-IN-7 (Compound 43b), an isochinoline derivative, functions as a potent dual inhibitor of IDO1 TDO with IC50 values of 0.31 μM and 0.08 μM, respectively. Demonstrating favorable pharmacokinetics and strong antitumor efficacy in the B16-F10 tumor model, this compound also exhibits low toxicity.

D5B is an effective and selective PD-L1 inhibitor that has been modified with DBCO. It degrades PD-L1 in 4T1 and B16-F10 tumor cells with EC50 values of 5.4 μM and 6.2 μM, respectively. D5B can block the PD-L1 PD-1 interaction and exhibits antitumor activity.

Microtubule inhibitor 12 (Compound 2k) is a microtubule polymerization inhibitor with an IC50 of 22.23 μM. It causes cell cycle arrest at the G2 M phase in B16-F10 cells, induces apoptosis, and impedes cell migration. This compound inhibits the proliferation of cancer cells B16-F10, A549, HepG2, and MCF-7 with IC50 values of 0.098, 0.135, 0.109, and 0.259 μM, respectively, and demonstrates antitumor activity in mouse models.

PD-L1 HDAC6-IN-1 (Compound HP29) is an inhibitor targeting both PD-L1 and HDAC6, effectively disrupting the PD-L1 PD-1 interaction and inhibiting HDAC6 activity, with IC50 values of 26.8 nM and 69 nM, respectively. This compound enhances the cytotoxicity of Jurkat T cells against HepG2 cells, exhibiting an IC50 of 3.4 μM. In rats, PD-L1 HDAC6-IN-1 demonstrates favorable pharmacokinetics, showing a drug exposure level of 871.62 ng·h mL, and displays antitumor activity in a B16-F10 xenograft mouse model.

BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.

Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg ml, respectively). It is cytotoxic to B16 F10 and Moser cells (IC50s = 0.0008 and 0.04 μg ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).

CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

DMHAPC-Chol is a cationic cholesterol. Liposomes containing DMHAPC-chol have been used for DNA plasmid delivery in vitro and in vivo in a B16-F10 mouse xenograft model. Liposomes containing DMHAPC-chol are cytotoxic to B16-F10 cells when used at lipid concentrations greater than 20 μM. DMHAPC-Chol, as part of a lipoplex with DOPE , has also been used to deliver DNA into mouse lung via intratracheal injection, resulting in a heterogeneous distribution in the bronchi and bronchioles, and to deliver VEGF siRNA into A431 and MDA-MB-231 cells, which secrete VEGF.

Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma model. 1.Morin, M.D., Wang, Y., Jones, B.T., et al.Diprovocims: A new and exceptionally potent class of toll-like receptor agonistsJ. Am. Chem. Soc.140(43)14440-14454(2018) 2.Wang, Y., Su, L., Morin, M.D., et al.Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in miceProc. Natl. Acad. Sci. U.S.A.115(37)E8698-E8706(2018)

93-O17S is a chalcogen-containing cationic lipidoid. It has been used in the synthesis of lipid nanoparticles (LPNs) for the delivery of Cre recombinase and ribonucleoproteins for genome editing in mice. LPNs containing 93-O17S have been utilized for the intratumoral delivery of cGAMP to enhance cross-presentation of tumor antigens and stimulation of interferon genes [STING] activation in a B16 F10 murine melanoma model.