a375

LXH254 is a potent C-Raf and B-Raf inhibitor.

RA375, an inhibitor of RPN13 (26S proteasome regulatory subunit), enhances UPR signaling, ROS production, and apoptosis. Demonstrating ten times the efficacy against cancer lines compared to RA190, RA375 owes its increased activity to nitro ring substituents and the inclusion of a chloroacetamide warhead.

1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res

Licochalcone D may be a potential drug for human melanoma treatment by inhibiting proliferation, inducing apoptosis via the mitochondrial pathway and blocking cell migration and invasion. Licochalcone D has cardioprotective potential against myocardial is

Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1 2 4 inhibitor (IC50: 4.7 18.7 1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line.

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).

Antiproliferative agent-13 is a compound with antiproliferative activity.

Sartorypyrone B, a 2β-acetoxyl analogue of chevalone C, is derived from the ethyl acetate extract of the culture of Neosartorya tsunodae (KUFC 9213), a fungus associated with marine sponges. This compound demonstrates potent growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cancer cell lines with GI50 values of 17.8, 20.5, and 25.0 μM, respectively, indicating its potential in the study of breast adenocarcinoma, non-small cell lung cancer, and melanoma [1].

Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate cancer cell growth through activation of cell apoptosis and downregulation of androgen receptor ex

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

Cedrusin shows a cytotoxic effect on A375 and HeLa cells.

Benzyl DC-81 (Compound 6a), an anticancer agent, exhibits antiproliferative activity against A375 and MCF-7 cells [1].

HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 µM in A375 cells).

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

GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).

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].

(–)-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.

RAF-IN-1 is a potent inhibitor of b/cRAF, acting on cRAF (IC50: 3.8 nM), bRAFwt (IC50: 36 nM), bRAFV600E (IC50: 29.4 nM) and inhibiting A375 and H358 cell lines carrying the bRAFV600E mutation with a GI50 of 3.4 and 2.9 nM.

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

Desacetylcinobufagin (Deacetylcinobufagin) , a natural product, shows potent activities against Hela and A375 cells in vitro.

DMU-212 is a methylated derivative of Resveratrol , with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active[1][2]. DMU-212 (0.3125-40 μM) inhibits growth of A375, MeWo, Bro and M5 cells human melanoma cells[1].DMU-212 (30-50 μM; 24 hours) induces upregulation of cell cycle inhibitors, apoptosis and ERK activation in A375 cells[1].DMU-212 induces upregulation of cell cycle inhibitors, apoptosis and ERK activation in A375 cells[1].DMU-212 induces G2/M arrest and apoptosis in cancer cells[1].DMU-212 induces mitotic arrest, apoptosis and activation of ERK1/2 protein[1]. Cell Proliferation Assay[1] Cell Line: A375 cells, MeWo cells, M5 cells, Bro cells DMU-212 (50 mg/kg; i.g.; three times a week; for 14 days) inhibits tumor growth in xenograft model of human ovarian cancer[2]. Animal Model: 6-weeks-old SCID female mice (20-24 g), with ovarian cancer xenografts[2] [1]. Vasilis Pericles Androutsopoulos, et al. Activation of ERK1/2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4. [2]. Hanna Piotrowska, et al. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400.

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

CAY10784 is a STAT3 inhibitor (IC50= 0.74 μM in a reporter assay) and a derivative of WP1066 .1It inhibits proliferation of HeLa, Caco-2, A549, A375, U87MG, and HL-60 cancer cells (IC50s = 1.8, 1.8, 3, 2.8, 2.3, and 1.2 μM, respectively) but not PC3 or HT-29 cancer cells (IC50s = >10 μM for both). CAY10784 is also active againstH. pyloriandC. jejuni(MICs = 1.6 and 4.7 μM, respectively).2 1.Lü, Z., Li, X., Li, K., et al.Structure-activity study of nitazoxanide derivatives as novel STAT3 pathway inhibitorsACS Med. Chem. Lett.(2021) 2.Ballard, T.E., Wang, X., Olekhnovich, I., et al.Synthesis and antimicrobial evaluation of nitazoxanide-based analogues: Identification of selective and broad spectrum activityChemMedChem6(2)362-377(2011)

PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferative activity against A375 cells [1].

MEK-IN-6 hydrate (compound 69), a MEK inhibitor, exhibits an IC50 value of 2 nM in A375 cells [1].

MEK-IN-6 (Example 69), a potent MEK inhibitor, effectively inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells, with an IC50 of 2 nM, making it valuable for cancer research [1].

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

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.

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research[1]. ARN-21934 display a different affinity for topoIIα and topoIIβ. ARN-21934 is more potent against the α isoform, the IC50 value for the inhibition of DNA relaxation by topoIIα is 2 μM, the value for inhibition of DNA relaxation by topoIIβ is 120 μM[1].ARN-21934 exhibits a small panel of human cancer cell lines. It against melanoma (A375 and G-361), breast (MCF7), endometrial (HeLa), lung (A549), and androgen-independent prostate (DU145) cancer cells with IC50 values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively[1]. ARN-21934 (intraperitoneal injection; 10 mg/kg; single dose) reaches a maximal plasma concentration of 0.68 μg/mL after 15 min. The half-life is 149 min in circulation, still being present in plasma 360 min after injection. The compound also exhibits good clearance values (0.116 L/(min kg)). Besides, ARN-21934 is able to reach the brain, with a maximum concentration of compound at 60 min, and is still present in the brain 360 min after injection[1] [1]. Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.

SHR902275 is a selective, potent, orally active RAF inhibitor capable of targeting RAS mutant cancers. SHR902275 acts on cRAF (IC50: 1.6 nM), bRAFwt (IC50: 10 nM), bRAFV600E (IC50: 5.7 nM). SHR902275 has cell growth inhibitory effects and acts on H358 cells (GI50: 1.5 nM), A375 cells (GI50: 0.17 nM), Calu6 cells (GI50: 0.4 nM) and SK-MEL2 cells (GI50: 0.32 nM).

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.

CX-5461 dihydrochloride is a potent, orally active inhibitor of Pol I-mediated rRNA synthesis that acts on HCT-116 cells (IC50: 142 nM), A375 cells (IC50: 113 nM) and MIA PaCa-2 cells (IC50: 54 nM), and to a lesser extent on Pol II (IC50 ≥ 25 μM).

ERK1/2 Inhibitor 9 (Probe 1), a covalent antagonist of ERK1/2, exhibits sub-micromolar efficacy in cellular assays (A375 GI50=0.47 μM) and facilitates the reduction of phospho-ERK1/2 levels. When conjugated with trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine-tagged Thalidomide), it forms the corresponding ERK-CLIPTAC, promoting targeted ERK1/2 degradation [1].

KPT-251 is a selective nuclear export inhibitor.

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).

Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and can be used to study hepatocellular carcinoma.

POL1-IN-1 (Compound 3A) can effectively inhibit the transcription of RNA polymerase I in the A375 malignant melanoma cell line but has no effect on polymerase II.

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.

LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.