b16f10

Methyl myristate (methyl tetradecanoate) is a natural product.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

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

Dexamethasone is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory, immunosuppressive, and apoptosis-inducing activities. It inhibits the production of inflammatory miRNA-155 exosomes in macrophages, significantly reduces inflammatory cytokine expression in neutrophils and monocytes, suppresses LPS-induced macrophage inflammation, and induces autophagy. It is commonly used to induce animal models of depression, muscle atrophy, and hypertension, and holds potential in COVID-19 research.

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.

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.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Thiabendazole (2-(4-Thiazolyl)benzimidazole) is a benzimidazole derivative with anthelminthic property.

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.

Capsaicin is an active natural component found in chili peppers and acts as a TRPV1 agonist (EC50 = 0.29 μM). It possesses multiple activities, including pain relief, antitumor, anti-inflammatory, antioxidant, and neuroprotective effects, as well as some neurotoxicity. Capsaicin can be used to establish itch models.

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

L-Kynurenine ((S)-Kynurenine) is an endogenous agonist of the tryptophan metabolite and the aromatic hydrocarbon receptor (AHR). L-Kynurenine can inhibit the proliferation of allogeneic T cells and increase the invasion of malignant U87 glioma cells into the collagen matrix.

(+)-Butin is the R-enantiomer of butin and exhibits potential anti-fertility activity. Butin is a natural flavonoid compound that is orally active and possesses significant antioxidant, antiplatelet, and anti-inflammatory effects.

Reticulol is an isocoumarin derivative produced by certain species of Streptomyces. Reticulol inhibits cAMP phosphodiesterase (IC50 = 41 µM). Recticulol (M.W. 222.2) exhibits a potent in vitro cytotoxicity against the human lung tumor cell line A427 and the mouse melanoma cell line B16F10.

Tyrosinase-IN-35 (compound 6g), exhibiting a IC 50 value of 2.09 μM, serves as a more effective inhibitor of human tyrosinase compared to Kojic Acid (IC 50: 16.38 μM). At concentrations of 4 μM and 8 μM, this compound effectively lowers melanin levels in melanoma B16F10 cells in vitro.

LD4172 is a PROTAC degrader capable of degrading RIP kinase (RIPK1) with a DC50 in the nanomolar range. When used in combination with TNF-α, LD4172 can induce apoptosis in B16F10 cells. In mouse models, it demonstrates antitumor activity. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL)

dPDL1-4 is a potent and selective eHSPTAC eHSP90PD-L1 degrader, with DC50 values of 7.77 μM (HeLa) and 6.52 μM (B16F10). It links eHSP90 to target proteins, inducing lysosomal degradation. dPDL1-4 effectively degrades PD-L1 and inhibits tumor growth, making it useful for research in cervical cancer and melanoma.

DeFer-2 is a ferritin PROTAC degrader (Kd= 17.1 μM). It triggers the degradation of ferritin leading to the accumulation of free iron ions and an increase in ROS, which subsequently initiates caspase 3-GSDME mediated pyroptosis in cancer cells. DeFer-2 significantly inhibits tumor growth and extends the survival of mice with subcutaneous B16F10 tumors, and it is useful for melanoma research.

PROTACRIPK1Degrader-1 is a selective RIPK1 PROTAC degrader. This compound degrades RIPK1 in various cancer cell lines, such as A375 and B16F10 cells. It enhances the anticancer effects of radiotherapy in both syngeneic and humanized mouse models. PROTACRIPK1Degrader-1 is applicable for research in cancers like melanoma.

PI3Kδ-IN-25 is an orally active and selective PI3Kδ inhibitor with an IC50 of 2.1 nM. It exhibits IC50 values of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. In B16F10 cells, PI3Kδ-IN-25 inhibits the phosphorylation of AKTSer473, suppresses Treg cell proliferation, and downregulates the expression of PD-L1. In mouse models of B16F10 melanoma and Lewis lung cancer, PI3Kδ-IN-25 demonstrates anticancer activity by reducing tumor-infiltrating Treg cells and enhancing immune responses. This compound is applicable for research on cancers such as melanoma and lung cancer.

STINGagonist-46 is an orally active STING agonist that activates the STING signaling pathway, leading to the phosphorylation of TBK1 and IRF3, and enhances the secretion of IFN-β and IP-10. It directly binds to STING, increasing its thermal stability. In B16F10, CT26, and 4T1 mouse models, STINGagonist-46 demonstrates potent antitumor efficacy. This compound can be utilized for research in cancer immunotherapy.

WZS0347 is a MITF PROTAC degrader. It effectively reduces MITF protein levels in several melanoma cell lines, including B16F10, A375, and GAK. WZS0347 significantly inhibits the proliferation, migration, and invasion of melanoma cells. This compound can be utilized for melanoma research.