b16f10

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

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.

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

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.

Methyl myristate (methyl tetradecanoate) is a natural product.

Methyl pentadecanoate is a natural product.

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)

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).

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].

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.

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.

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. It induces CDK4 6 degradation in B16F10 melanoma cells, arrests the cell cycle at the G0 G1 phase, and induces apoptosis. HEMTAC CDK4 6 degrader 1 can be used in cancer research [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].

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].

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].

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.

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

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].

RORγt agonist 4 (compound 14) acts as a potent and selective agonist for RORγt, significantly boosting metabolic stability. It also enhances the condition in mouse tumor models, specifically B16F10 melanoma and LLC lung adenocarcinoma [1].

Forsythoside F (Arenarioside) is a natural compound with GI50 values ranging from 10 to 16 μM against B16F10 cells.

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.

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

Citrostadienol shows cytotoxic activity against B16F10 melanoma cells.