melanoma

NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation.

Nicotinamide, a vitamin B3 derivative, is an inhibitor of SIRT1 (IC50=50-180 μM) and SIRT2 (IC50=2 μM). Nicotinamide can be used as a precursor of nicotinamide adenine dinucleotide or NAD+, which can be supplemented by dietary intake and can prevent or treat melanoglossia and pellagra.

"Methyl 4-hydroxycinnamate is an esterified derivative of p-coumaric acid isolated from the flowers of Trixis michuacana var. longifolia, exhibiting antibacterial and anti-melanogenesis properties."

N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with anti-melanoma activity. N6-Isopentenyladenosine, an RNA modification found in cytokinins, regulates plant growth/differentiation and improves the efficiency

3,4-Dihydroxybenzylamine hydrobromide (NSC-263475 hydrobromide) inhibits DNA polymerase activity in melanoma cells and displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.

BAY-985 is a potent, selective, and orally active ATP-competitive dual inhibitor of TBK1 and IKKε (IC50s: 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε) with antitumor efficacy.

Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) serves as a potent inhibitor related to Pentamidine, targeting the calcium-binding protein S100B with a dissociation constant (Kd) of 6.9 µM. It demonstrates specificity by preferentially killing melanoma cells overexpressing S100B compared to cells lacking this protein. Additionally, Heptamidine is employed as a valuable research tool in the study of Myotonic dystrophy (DM).

KPT-251 is a selective nuclear export inhibitor.

ζ-Stat (NSC37044), a specific and atypical inhibitor of PKC-ζ with an IC50 of 5 μM, demonstrates the ability to inhibit proliferation and induce apoptosis in melanoma cell lines, exhibiting antitumor activity in vitro[1][2].

Desmethylanethol trithione (ADT-OH) is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor. In the in vitro glucose-oxygen deprivation (OGD) model, Desmethylanethol trithione markedly attenuated tPA-enhanced Akt activation and VEGF expression in brain microvascular endothelial cells. Finally, Desmethylanethol trithione improved functional outcomes in mice subjected to MCAO and tPA infusion. H2S donors reduced tPA-induced cerebral hemorrhage by possibly inhibiting the Akt-VEGF-MMP9 cascade. Administration of H2S donors has potential as a novel modality to improve the safety of tPA following the stroke.

NMS-E973 is a potent and selective Hsp90 inhibitor with a DC50 of less than 10 nM for Hsp90 binding, displaying no activity against a panel of 52 diverse protein kinases.

Piclidenoson (CF-101), a selective agonist of adenosine A3 receptor(EC50 values of 0.11 μM), induces robust anti-inflammatory effect in psoriasis patients.

CCG-222740 is an inhibitor of Rho/MRTF pathway

AA92593 has been used as a selective inhibitor of melanopsin.

COH-SR4 (COH-SR4 (Mitochondria uncoupler SR4)) is a uncoupler of mitochondrial oxidative phosphorylation. COH-SR4 modulates amp-dependent kinase (ampk)-mammalian target of rapamycin (mtor) signaling, and inhibiting proliferation of hepg2 hepatocarcinoma cells

KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.

TBAP-001 is a RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay and an IC50 of 18 nM in Cell-Based Phosho-ERK Assay.

Picrocrocin is a natural product

Dacarbazine (DTIC-Dome) is an antineoplastic agent. It has significant activity against melanomas.

Oglufanide (H-Glu-Trp-OH) is a naturally occurring thymic immunomodulator that inhibits vascular endothelial growth factor (VEGF).

ATM-3507 trihydrochloride is a potent tropomyosin inhibitor (IC50s: 3.83-6.84 μM in human melanoma cell lines).

4'-bromo-Resveratrolis a potent inhibitor of the deacetylases sirtuin 1 (SIRT1) and 3 (SIRT3)

CAY10526 (BTH) is a selective mPGES-1 inhibitor that acts as an inhibitor of the NF-κB signaling pathway.

1. Chelidonine (Stylophorin) isolated from Chelidonium majus efficiently induced apoptosis in HeLa cells through possible alteration of p38-p53 and AKT/PI3 kinase signalling pathways. 2. Chelidonine is a promising model compound for overcoming MDR and for enhancing cytotoxicity of chemotherapeutics, especially against leukaemia cells, its efficacy needs to be confirmed in animal models. 3. Chelidonine may be a potential therapeutic agent against metastasis of invasive human cancer cells, exhibits antimigratory and antiinvasive effects in MDA-MB-231 cells, by suppressing COL-induced integrin signaling, through inhibiting the formation of the IPP complex and subsequent downregulation of IPP downstream signaling molecules, such as Akt and ERK1/2.