sw620

iFSP1, a potent, selective, and glutathione-independent ferroptosis suppressor protein 1 (FSP1) (AIFM2) inhibitor with an EC50 of 103 nM, sensitizes diverse human cancer cell lines to ferroptosis inducers like (1S,3R)-RSL3. It uniquely triggers ferroptosis in GPX4-knockout cells overexpressing FSP1.

SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.

Panaxadiol (20(R)-Panaxadiol) is a novel antitumor agent extracted from the Chinese medicinal herb Panax ginseng.

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Valspodar (PSC 833), a specific P-glycoprotein inhibitor and MDR regulator, is commonly used as a chemical sensitizer in the study of advanced epithelial ovarian cancer.

AG14361 is an effective inhibitor of PARP1 (Ki<5 nM).

Genistein (NPI 031L) is a naturally occurring soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor, antioxidant, and anthelmintic properties, and also produces estrogen-like effects in the body.

Urolithin A is a natural product, a metabolite of ellagic acid, which inhibits DNA synthesis and induces apoptosis and autophagy. Urolithin A exhibits antioxidant, anti-inflammatory and antitumor activities.

DL-Isoleucine exhibits anti-glycation activity in RAW 264.7 cells and exhibits millimolar-level cytotoxicity against SW620, CACO2, SW480, and fibroblast cells.

Compound 1T-0216 is a blocker of AKT1-FAK interactions and reduces stimulation of FAK phosphorylation by extracellular stress in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

PROTAC K-Ras Degrader-3 is a PROTAC degrader targeting K-Ras, exhibiting a DC50 value of ≤ 1 nM against SW620 KRAS G12D and a GI50 value of ≤ 10 nM in inhibiting the growth of SW620 3D cells. It is used in cancer research.

KRAS inhibitor-37 (compound 2) is a potent inhibitor of KRAS, exhibiting low dissociation constants (KD) with various KRAS mutations: wild type (0.004 nM), G12D (0.041 nM), G12C (0.019 nM), and G12V (0.144 nM). This compound effectively inhibits cell proliferation, demonstrating half-maximal inhibitory concentrations (IC50) ranging from <2 nM to 14 nM in H358, SW620, and PANC08.13 cell lines. KRAS inhibitor-37 holds potential for cancer research applications.

PROTAC K-Ras degrader-2 (compound 48) is a broad-spectrum KRAS mutant PROTAC degrader that demonstrates an IC50 of ≤200 nM for KRAS G12V/RAF1. Additionally, PROTAC K-Ras degrader-2 achieves a DC50 of ≤200 nM in degrading SW620 KRAS G12D and inhibits the growth of SW620 3D cells with an IC50 of ≤20 nM.

KRAS inhibitor-27 (Compound 15h) is a KRAS inhibitor that effectively targets KRAS G12D/G12V mutated cells (AsPC-1 and SW620) and wild-type KRAS cells (HT-29), with IC50 values of 378 nM, 0.6 nM, and 3230 nM, respectively. It reduces ERK phosphorylation, with IC50 values of 0.6 nM and 1 nM in AsPC-1 and SW620 cells, respectively, and decreases DUSP4 expression, thereby inhibiting the MAPK signaling pathway.

PROTAC K-Ras Degrader-4 (Compound 4) is a proteolysis-targeting chimera (PROTAC) molecule designed to selectively degrade oncogenic mutants of K-Ras, effectively degrading KRASG12D in the GP5d cell line and KRASG12V in SW620 cells with DC50 of 1 nM and 13 nM, respectively; it concomitantly inhibits the downstream MAPK signaling pathway and represents a novel therapeutic strategy for cancer research targeting previously undruggable Ras mutations.

KRAS inhibitor-41 is a KRAS inhibitor with an IC50 value of less than 0.01 μM for both KRAS G12D and KRAS G12V mutations. It effectively inhibits RAS mutant cell lines GP2D (KRAS-G12D) and SW620 (KRAS-G12V). KRAS inhibitor-41 is applicable for cancer research.

CDK9/EZH2-IN-1 is a dual-target inhibitor of CDK9 and EZH2 with IC50 values of 83.9 nM and 108.6 nM, respectively. It induces apoptosis and causes DNA double-strand breaks (DSB). Additionally, CDK9/EZH2-IN-1 inhibits the proliferation of MKN45, MDA-MB-453, and SW620 cancer cells, with respective IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM.

PRDX1-IN-2 (compound 15) is a selective inhibitor of the antioxidant enzyme Peroxiredoxin 1 (PRDX1) with an IC50 of 0.35 μM. It reduces mitochondrial membrane potential in SW620 cells, potentially due to increased ROS resulting from PRDX1 inhibition, leading to apoptosis. PRDX1-IN-2 is applicable in colorectal cancer research.

PROTACSOS1 degrader-10 (Compound 11o) is a degrader of son of sevenless 1 (SOS1) that functions through CRBN- and protease-dependent mechanisms. It effectively degrades SOS1 in KRAS-mutated cancer cells SW620, A549, and DLD-1, with DC50 values of 2.23, 1.85, and 7.53 nM, respectively. Additionally, PROTACSOS1 degrader-10 inhibits the proliferation of SW620, A549, and DLD-1 cells, with IC50 values of 36.7, 52.2, and 107 nM, and suppresses ERK phosphorylation.

TT2-32 TFA induces a biphasic activation of phosphotyrosine phosphatase activity in human colon tumor cell line, SW620

Previridicatumtoxin is a fungal metabolite that has been found inP. aethiopicumand has diverse biological activities.1,2It is an intermediate in the biosynthesis of the mycotoxin viridicatumtoxin . Previridicatumtoxin is active against methicillin-resistantS. aureus(MRSA) and vancomycin-resistantE. faecalis(IC50s = 4.4 and 4.8 μM, respectively), as well asC. albicansandS. cerevisiae(MIC = 32 μg/ml for both).2,1It is cytotoxic to NCI H460, KB-3-1, and SW620 cancer cells (IC50s = 5.3, 4.1, and 6 μM, respectively).2 1.Chooi, Y.H., Wang, P., Fang, J., et al.Discovery and characterization of a group of fungal polycyclic polyketide prenyltransferasesJ. Am. Chem. Soc.134(22)9428-9437(2012) 2.Shang, Z., Salim, A.A., Khalil, Z., et al.Viridicatumtoxins: Expanding on a rare tetracycline antibiotic scaffoldJ. Org. Chem.80(24)12501-12508(2015)

Amycolatopsin A is a macrolide polyketide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 0.4 and 4.4 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin A is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 0.08 and 1.2 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)