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.

Mertansine (DM1) refers to the thiol-containing maytansinoid, DM1 (N2'-deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine) attached to a monoclonal antibody through reaction of the thiol group with the SPP (N-succinimidyl 4-(2-pyridyldithio)) linker to create an antibody-drug conjugate or ADC. Experimental ADCs with the SPP-DM1 design include lorvotuzumab mertansine.

Methyl pentadecanoate is a natural product.

Methyl myristate (methyl tetradecanoate) is a natural product.

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).

Forsythoside F (Arenarioside) is a natural product, and GI50 values of 10-16 microM against B16F10 cell.

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.

Chlorophorin shows high anti-protozoal activity with an MIC of 0.25 microg/ml. Chlorophorin can strongly inhibit mushroom tyrosinase activity with IC50 values of 2.5 ± 0.408 uM; it inhibits α-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells.

GB 2a shows antioxidant and anti-inflammatory effects, it can prevent the carrageenan-induced paw oedema. GB 2a biflavonoid can promote inhibition on tyrosinase activity and reduced melanin biosynthesis in B16F10 cells, which suggests great potential for

Citrostadienol shows cytotoxic activity against B16F10 melanoma cells.

Dual photoCORM 1 (compound 5), a metal-free, photoactive, dual carbon monoxide releasing molecule (CORM), demonstrates efficient cellular uptake and enables real-time tracking of CO release via a colorimetric change in B16F10 cancer cells [1].

TT-012 has anti-tumor activity, selectively binds dynamic MITF and disrupts the dimer formation and DNA binding of the latter. TT-012 can inhibit the transcription of MITF in B16F10 melanoma cells. TT-012 inhibited the growth and metastasis of MITF melanoma cells in animal models. TT-012 is less cytotoxic to liver and immune cells.

PRL-3 Inhibitor I (BR-1) is a phosphatase of regenerating liver 3 (PRL-3) inhibitor which blocks the migration and invasion of metastatic cancer cells.

APBC is a novel PD-L1 inhibitor, effectively interrupting the PD-1/PD-L1 interaction by directly binding to PD-L1, presenting the KD and IC50 values at low-micromolar level, displaying superior antitumor efficacy in hPD-L1 knock-in B16F10-bearing mouse model without the induction of observable liver toxicity.

Syringetin, a flavonoid derivative found in grapes and wine, promotes melanogenesis in B16F10 cells and inhibits osteoblast-mediated osteoclastogenesis in human lung adenocarcinoma.

CCZ01048 TFA, an α-MSH analogue, demonstrates a strong binding affinity for the melanocortin 1 receptor (MC1R), displaying a K i value of 0.31 nM. It exhibits rapid internalization into B16F10 melanoma cells and maintains high in vivo stability. CCZ01048 TFA holds potential as an effective agent for PET imaging of malignant melanoma [1].

CCZ01048, an analogue of α-melanocyte-stimulating hormone (α-MSH), demonstrates a high binding affinity for the melanocortin 1 receptor (MC1R), with a Ki of 0.31 nM. It rapidly internalizes into B16F10 melanoma cells and exhibits notable in vivo stability, making it a promising candidate for PET imaging of malignant melanoma [1].

6-O-Isobutyrylbritannilactone, a sesquiterpene natural melanogenesis inhibitor, can be extracted from Inula britannica flowers. It effectively suppresses IBMX-induced melanin production in B16F10 cells and exerts antimelanogenic effects in zebrafish embryo models by modulating ERK, PI3K/AKT, and CREB pathways [1].

HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a K d value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis . HEMTAC CDK4/6 degrader 1 can be used in research of cancer [1] .

DMGF, also known as 7,7-dimethoxyagastisfavone, is a biflavonoid isolated from Taxus × media cv. Hicksii. DMGF induces apoptotic and autophagic cell death. DMGF could effectively attenuate the motility of B16F10 cells, and the results of real-time PCR revealed that DMGF also suppressed the expressions of matrix metalloproteinase-2 (MMP-2). MGF can inhibit the metastasis of highly invasive melanoma cancer cells through the down-regulation of F-actin polymerization DMGF may be further developed to serve as a chemoprevention drug for patients with metastatic melanoma.

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

Tyrosinase-IN-13 (compound 3c), stemming from Flurbiprofen, acts as a potent non-competitive inhibitor of tyrosinase, exhibiting IC50 and Ki values of 68 μM and 36.3 μM respectively. This compound demonstrates cytotoxicity against several cancer cell lines, including hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) [1].

Melanoma is a lethal skin cancer. The early detection of melanoma using positron emission tomography (PET) probes is critical for improving the survival of melanoma patients. Melanin probe-2 is a non-radioactive bromo-picolinamide precursor that has been used for the synthesis of18F-picolinamides based PET probe (melanin probe-1). The tumor-targeting efficacy and imaging property of three melanin probes were evaluated in B16F10 tumor-bearing mice.18F-1 and18F-3 had much lower tumor uptake compared with18F-2 (Melanin probe-2), which were 12.74 ± 1.70, 16.61 ± 2.60, and 16.87 ± 1.23 %ID/g at 0.5, 1, and 2 h, respectively[1].