melanoma cell growth

4'-Bromo-resveratrol 是Sirtuin-1和Sirtuin-3的双重抑制剂。它通过线粒体代谢重编程，使黑色素瘤细胞的生长受到抑制。它通过代谢重编程、影响细胞周期以及细胞凋亡的信号传导，使其在黑色素瘤细胞中发挥抗增殖作用。

Sabizabulin (ABI-231)是一种有效、具有口服生物利用度的 α 和 β 微管蛋白抑制剂，可对抗黑色素瘤和前列腺癌细胞系。 Sabizabulin 能通过靶向 HPV E6 和 E7 抑制宫颈癌细胞的肿瘤生长和转移表型同时还能用于前列腺癌的研究。

ND-322 HCl (ND 322 Hydrochloride) 是 MT1-MMP 和 MMP2 的选择性抑制剂，可减少体外黑色素瘤细胞的生长、迁移和侵袭。

3,4-Dihydroxybenzylamine hydrobromide (NSC-263475 hydrobromide) 抑制黑色素瘤细胞中的 DNA 聚合酶活性，并在具有不同程度酪氨酸酶活性的黑色素瘤细胞系中显示出生长抑制活性。

EOAI3402143 是一种去泛素化酶抑制剂，以剂量依赖性抑制 Usp9x Usp24和 Usp5，增加肿瘤细胞凋亡。

Mensacarcin, a highly complex polyketide compound, exhibits multifaceted effects on cellular processes. Specifically, it targets mitochondria, perturbs energy metabolism within these organelles, and activates caspase-dependent apoptotic pathways. Functionally, Mensacarcin can serve as a cytotoxic constituent in antibody-drug conjugates (ADCs). Furthermore, this antibiotic compound displays broad-spectrum inhibition of cell growth across various cancer cell lines and demonstrates potent induction of apoptosis in melanoma cells.

经化学修饰的四环素 （CMTs） 可抑制 MMPs，但缺乏抗菌活性。四环素的非抗菌衍生物称为 incyclinide (COL-3, CMT-3)。 实验证明，Incyclinide（CMT-3） 可抑制前列腺癌、结肠腺癌和黑色素瘤在细胞培养中的侵袭性，并抑制肿瘤的生长和转移。

UC-112是凋亡抑制蛋白IAP 新型高效抑制剂，癌细胞IC50值0.7-3.4uM。

SIJ1777作为GNF-7的衍生物，对携有BRAFI II III类突变的黑色素瘤细胞展现出显著的抗癌效果。该化合物有效抑制了MEK、ERK和AKT的活化，极大地诱导了细胞凋亡(apoptosis)。此外，SIJ1777也有效阻断了带BRAFI II III突变的黑色素瘤细胞的迁移、侵袭及锚定非依赖性生长。

CHI-KAT8i5 是一种高选择性的KAT8抑制剂，具有 19.72 μM 的 KD。它能以剂量依赖性方式引发凋亡 (Apoptosis)，并抑制食管鳞状细胞癌、结肠癌、黑色素瘤、胃癌、非小细胞腺癌及肝癌的肿瘤生长。

NSC49652 在神经元和黑色素瘤细胞中触发依赖于 p75NTR 和 JNK 活性的凋亡细胞死亡，并抑制黑色素瘤小鼠模型中的肿瘤生长。

AMG-628 is an effective and ATP-competitive RAF kinase inhibitor. AMG-628 has been shown to inhibit growth and induce cell cycle arrest and apoptosis in colon and melanoma cell lines with B-RAFV600E mutations.

Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit

Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto 5′ nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg ml) and Gram-negative bacteria (MICs = 136-200 µg ml), as well as yeasts (MICs = 10-20 µg ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16 BL6 mouse model of melanoma when administered at a dose of 25 mg kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg kg.3Ajoene (25 mg kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16 BL6 melanoma cells in C57BL 6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

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).

DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物，表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1 2蛋白阻止有丝分裂。

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respectively). Chromomycin A2 (30 nM) halts the cell cycle in the G0 G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells, indicating that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50= 30 nM).1It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 μM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 μM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 μM). BX-320 (200 mg/kg) inhibits the growth of lung tumors in a LOX melanoma mouse model of blood-borne metastasis. 1.Feldman, R.I., Wu, J.M., Polokoff, M.A., et al.Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1J. Biol. Chem.280(20)19867-19874(2005)

ACA-28 (compound 2a) 是ERK MAPK 信号的有效调节剂，可通过过度激活 ERK 诱导细胞凋亡，从而选择性抑制癌细胞生长。ACA-28 对黑色素瘤细胞 (SK-MEL-28) 和正常黑色素细胞 (NHEM) 细胞生长的IC50值分别为 5.3 和 10.1 μM。

AMG-628, (S)-, is the S isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.

AMG-628, (R)- is the R isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.

Nicotinamide Hydrochloride 是维生素 B3 或烟酸的一种形式，可抑制SIRT2的体外活性，其EC50值为 2 μM。 Nicotinamide Hydrochloride 可抑制 90% 的黑色素瘤细胞数量，并增加细胞内 NAD+、ATP、ROS 水平。Nicotinamide Hydrochloride 抑制黑色素瘤小鼠的肿瘤生长并提高生存率，可用于黑色素瘤等皮肤癌相关的研究。