a375

LXH254 是B/C RAF 抑制剂。

Nicotinamide 是维生素 B3 的吡啶核苷形式，可作为烟酰胺腺嘌呤二核苷酸或 NAD+ 的前体，可通过膳食摄入来补充，能预防或治疗黑舌病和糙皮病。

RA375 是一种 RPN13（26S 蛋白酶体调节亚基）抑制剂。 RA375 激活 UPR 信号、ROS 产生和细胞凋亡。 RA375 对癌症细胞的活性比 RA190 高 10 倍，这反映了它的硝基环取代基和氯乙酰胺弹头的添加。

Licochalcone D 是一种 NF-κB p65的有效抑制剂，是一种存在于 Glycyrrhiza inflate 中的黄酮类化合物，具有抗氧化、抗炎、抗癌等作用。

Atractylenolide I 是从白术根中得到的一种倍半萜烯，具有神经保护、抗过敏、抗炎和抗癌等多种生物活性。它是一种TLR4拮抗剂，在 A375 细胞中，能够降低JAK2和STAT3的磷酸化水平。

Rotundic acid (Rutundic acid) 是一种从圆形肠球菌中获得的三萜类天然产物，具有抗炎和保护心脏的能力。它可通过 AKT mTOR 和 MAPK 途径在肝细胞癌中诱导 DNA 损伤和细胞凋亡。

JNK-IN-8 (JNK Inhibitor XVI) 是一种有效的JNK 抑制剂，抑制JNK1、JNK2和JNK3，IC50分别为 4.7、18.7 和 1 nM。

PROTAC BRAF-V600E degrader-1 (Compound 23) 选择性地诱导 BRAF-V600E 的降解，而不是野生型 BRAF。

Antiproliferative agent-13是一种具有抗增殖活性的化合物。

ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。

POL1-IN-1 (Compound 3A) 是一种RNA 聚合酶 1 POL1抑制剂，IC50值低于 0.5 uM。 它能有效抑制A375恶性黑色素瘤细胞系中RNA 聚合酶I 的转录。

HLM006474 是光谱的E2F 抑制剂，在 A375 细胞中，可抑制 E2F4 DAN 结合(IC50:29.8 µM)。

GDC-0623 (RG 7421) 是一种 ATP 竞争性的MEK1抑制剂，Ki 值为 0.13 nM。它对 A375 细胞中 BRAFV600E 的 EC50值为 7 nM，而对 HCT116 细胞中 KRAS (G13D)的 EC50值为 42 nM。

CAY10526 (BTH) 是 mPGES-1 的选择性抑制剂，可抑制 NF-κB 信号通路。

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。

Desacetylcinobufagin (Deacetylcinobufagin) 是一种天然化合物，可用于微生物转化。

CAY10784 (STAT3-IN-17) 是一种 STAT3 抑制剂，具有抗增殖活性和抗肿瘤活性。CAY10784 对艰难梭菌显示出抗菌活性。

LY3009120 (DP-4978) 是一种泛RAF 抑制剂，其抑制BRAFV600E、BRAFWT 和CRAFWT 的IC50分别为 5.8、9.1和15 nM。

KPT-251 是一种选择性核输出抑制剂。

ST-168 is a potent inhibitor of PI3K and MEK. ST-168 displays improved PI3K and MEK1 isoform inhibition. ST-168 demonstrated a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ isoforms and a 2.2-fold improvement

Benzyl DC-81 (Compound 6a) 是一种抗癌化合物，展现对A375和MCF-7细胞线具有显著的抗增殖作用。

EPZ020411是一种特异性有效的 PRMT6 抑制剂， IC50 为 10 nM，比作用于 PRMT1 和 PRMT8 的选择性高10倍多。

hDHODH-IN-9 (Compound 3k) is a highly potent inhibitor of hDHODH, exhibiting an IC50 of 0.34 μM. It displays significant cytotoxic activity against MCF-7 and A375 cells, while maintaining good selectivity. With its characteristics, hDHODH-IN-9 holds promise for cancer disease research [1].

RAF-IN-1 是 b cRAF 的有效抑制剂，能够作用于 cRAF (IC50: 3.8 nM)、bRAFwt (IC50: 36 nM)，bRAFV600E (IC50: 29.4 nM)，能够抑制携带 bRAFV600E 突变的 A375 和 H358 细胞系，其 GI50分别为 3.4 和 2.9 nM。

(–)-Voacangarine, an indole alkaloid isolated from V. africana, exhibits cytotoxicity towards various cell lines including HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 values of 20 µg ml. Additionally, it demonstrates cytostatic effects on wild-type S. cerevisiae and is cytotoxic to Δrad3-e5 and Δrad6-1 mutant strains of S. cerevisiae, which have defects in DNA strand break repair and the mutagenic repair pathway, respectively.

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).

MSG606 TFA, a potent antagonist of the human MC1 receptor (IC50 = 17 nM), functions as a partial agonist at the human MC3 and MC5 receptors (EC50 values of 59 and 1300 nM, respectively). It demonstrates binding affinity for A375 melanoma cells in vitro and selectively reverses induced hyperalgesia in female mice without affecting male mice.

MEK-IN-6（Example 69）是一种针对MEK的抑制剂，在A375细胞中有效抑制ERK1/2（THR202/Tyr204）的磷酸化，其IC50值为2 nM。此化合物主要应用于癌症研究领域。

MEK-IN-6 hydrate（compound 69）为MEK抑制剂，其对A375细胞展现出强效性，IC50仅为2 nM。

PROTACMEK1Degrader-1是一种针对MEK1的PROTAC，显示出pIC50值为7.0。该化合物由MEK1抑制剂与von Hippel-Lindau配体构成，能够抑制ERK1 2的磷酸化，并对A375细胞展现出抗增殖活性。

CX-5461 dihydrochloride 是一种有效的、口服具有活力的 Pol I 介导的 rRNA synthesis 抑制剂，能够作用于 HCT-116 细胞 (IC50: 142 nM)，A375 细胞 (IC50: 113 nM) 和 MIA PaCa-2 细胞 (IC50: 54 nM)，对 Pol II 作用较小 (IC50≥25 μM)。

Aszonapyrone A is a meroditerpene fungal metabolite that has been found in Neosartorya and has diverse biological activities.1,2,3 It inhibits the growth of MCF-7, NCI H460, and A375-C5 cancer cells (GI50s = 13.6, 11.6, and 10.2 μM, respectively).1 Aszonapyrone A is active against multidrug-resistant isolates of S. aureus, E. faecalis, and E. faecium (MICs = 8, 16, and 16 μg/ml, respectively) and inhibits S. aureus biofilm formation.2 It is also active against P. falciparum in vitro (IC50 = 1.34 μg/ml).3

EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases including BRK, FGFR1, c-Kit, and PDGFRb.

SHR902275 是选择性的、有效的、口服具有活力的 RAF 抑制剂，能够靶向 RAS 突变癌症。 SHR902275 能够作用于 cRAF (IC50: 1.6 nM)、bRAFwt (IC50: 10 nM)、bRAFV600E (IC50: 5.7 nM)。SHR902275 具有细胞生长抑制效果，能够作用于 H358 细胞 (GI50: 1.5 nM)、A375 细胞 (GI50: 0.17 nM)、Calu6 细胞 (GI50: 0.4 nM) 和 SK-MEL2 细胞 (GI50: 0.32 nM)。

ARN25062 是 Cdc42 和 p21 活化激酶（PAK）蛋白相互作用抑制剂。ARN25062 抑制 SKM28、SK-MEL-3、WM3248、 A375 和 SW480 细胞的增殖（IC50s=6.1、4.6、9.3、5.1和5.9 µM）。

Ocotillone has potent antibacterial activity against Gram-negative bacteria, P. aeruginosa and S. typhimurium, that are without hemolytic activity, whereas it has weak antimicrobial activity against Gram-positive bacteria and fungi. Ocotillone shows only

Sartorypyrone B为Chevalone C的2β-乙酰氧基衍生物，由海绵源真菌Neosartorya tsunodae(KUFC 9213)的培养物中乙酸乙酯提取得到。该化合物对MCF-7、NCI-H460和A375-C5细胞系展示出较强的生长抑制活性，GI50s值分别为17.8、20.5和25.0 μM，显示其在乳腺癌、非小细胞肺癌和黑色素瘤研究中的应用潜力。

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).

ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme). It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide and C16 ceramide in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 μM, respectively).

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC50 = 91, 3.4, 466, and 28 μM, respectively). PI3Kα inhibitor 2 inhibits A375 melanoma cell proliferation with an IC50 value of 580 nM.

Combretastatin A-1 是一种有效的微管抑制剂，具有抗肿瘤和抗血管活性，通过微管蛋白解聚介导的 AKT 失活抑制 Wnt β-catenin 通路发挥作用，可用于研究肝癌。

Cedrusin shows a cytotoxic effect on A375 and HeLa cells.

ERK1/2 inhibitor 9 (Probe 1)为共价ERK1/2抑制剂，具备亚微摩尔级别的细胞活性(A375 GI50=0.47 μM)，能够下调磷酸化ERK1/2。通过与反式环辛烯(TCO)标记的Tz-Thalidomide相结合，ERK1/2 inhibitor 9可形成ERK-CLIPTAC，进而触发ERK1/2的降解。