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。

OB 24 hydrochloride是一种选择性和口服活性的HO-1抑制剂(IC50=1.9 μM），具有抗肿瘤和抗转移性，可用于研究前列腺癌黑色素瘤、卵巢癌和肺癌转移等。

FJ9是一种有效的Wnt/β-catenin拮抗剂(Ki=29 μM)，能够下调典型Wnt信号传导，抑制HSC(肝星状细胞)活化和降低MeCP2蛋白。FJ9还能够破坏Frz7与DVL PDZ 结构域之间的蛋白质相互作用，诱导人癌细胞系凋亡和抑制小鼠异种移植瘤模型中的肿瘤生长。

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。

SR-2890（化合物 SR-2890） 是一种强效、高选择性酪蛋白激酶 1δ/1ε(CK1δ/ε )抑制剂，对 CK1δ 的IC50值为4 nM。该化合物在MTT实验中以38 nM的EC50值抑制黑色素瘤A375细胞生长，具有适用于人类癌细胞系异种移植研究的药代动力学特性。

GJ19 是一种 PD-L1 抑制剂，IC50 值为 32.06 nM。GJ19 能与人源及鼠源 PD-L1 蛋白紧密结合，KD 值分别为 171 nM 和 290 nM。在 HepG2/hPD-L1 和 Jurkat T/hPD-1 细胞共培养模型中，GJ19 对 HepG2 细胞表现出浓度依赖性促细胞死亡的作用。在 B16-F10 黑色素瘤小鼠模型中，GJ19 显示出显著的肿瘤生长抑制效果。此化合物适用于研究肿瘤免疫治疗。

IKP-104 是一种微管/微管蛋白 (microtubule/tubulin) 抑制剂，具有 IC50 值为 1.31 μM。通过抑制微管合成并诱导细胞骨架微管解聚，IKP-104 能够阻止细胞进展到有丝分裂期和 M 期。它有效抑制小鼠和人类肿瘤细胞系的生长，并对小鼠腹水瘤及肺癌模型展现抗肿瘤活性。IKP-104 还可用于研究白血病、肺癌和黑色素瘤等癌症。

Tubulin polymerization-IN-84 可通过靶向秋水仙碱结合口袋，实现对微管蛋白（Tubulin）聚合过程的抑制，其抑制作用的IC50值为10.9 μM。Tubulin polymerization-IN-84 对Jurkat、B16-F10、HCT116及MDA-MB-231四种细胞均表现出抗增殖活性，对应的IC50值分别为60 nM、380 nM、138 nM和1.054 μM。在B16-F10细胞中，Tubulin polymerization-IN-84能够诱导细胞发生G2/M期周期阻滞，并进一步触发细胞凋亡（apoptosis）。此外，在B16-F10黑色素瘤模型中，可有效抑制肿瘤组织的生长；当与PD-L1单克隆抗体联合使用时，还能增强体内抗肿瘤免疫应答，可用于T细胞急性淋巴细胞白血病、黑色素瘤、结肠癌以及乳腺癌的相关研究领域。

NHI-2 是一种乳酸脱氢酶 A (LDHA) 抑制剂，其 IC50 值为 14.7 µM，对 LDHB 的 IC50 为 55.8 µM，对 LDHA 有高选择性。NHI-2 作为高效的抗糖酵解剂，可增强细胞凋亡、诱导 S 和 G2 期细胞周期阻滞，并在癌细胞中产生广谱抗增殖作用。NHI-2 还影响细胞外酸化速率及 ATP 生成，并在小鼠 B78 黑色素瘤模型中显示肿瘤生长抑制效果，凸显其在癌症代谢研究中的作用。

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)

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.