sw620

Panaxadiol (20(R)-Panaxadiol) 是从人参根中获得，具有神经保护和抗肿瘤作用，能够抑制程序性细胞死亡配体-1(PD-L1)的表达和肿瘤增殖。

iFSP1 是一种强效、选择性和谷胱甘肽独立的铁死亡抑制蛋白 1 (FSP1) (AIFM2) 抑制剂，具有EC50 为 103 nM。它能够使多种人类癌细胞系对铁死亡诱导剂敏感，例如 (1S,3R)-RSL3。它在过表达 FSP1 的 GPX4 敲除细胞中选择性地诱导铁死亡。

Sertindole (Lu 23-174) 是一种非典型抗精神病药，可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合，Kd 值分别为 2.7、20、0.14 和 6 nM。

SAR-020106 是一种强效、ATP 竞争性和选择性 CHK1 抑制剂，IC50为 13.3 nM。它对 CHK2 具有良好的选择性，可通过选择抗癌药物增强抗肿瘤活性。

LP-261 是一种新型的微管蛋白靶向抗癌剂，可与微管蛋白上的秋水仙碱位点结合，诱导 G2 M 期阻滞，其EC50为 3.2 μM。它可抑制人非小细胞肺癌的生长，可用于癌症研究。

Oxaliplatin (L-OHP) 是一种 DNA 烷化剂，一种 DNA 合成抑制剂。Oxaliplatin 会导致 DNA 交联损伤，阻止 DNA 复制和转录并导致细胞死亡。Oxaliplatin 可以诱导细胞自噬。

Valspodar (PSC 833) 是一种特异性的 P-糖蛋白抑制剂和MDR调节剂，常被用作化学增敏剂，可用于研究晚期上皮卵巢癌。

Genistein (NPI 031L) 属于天然的大豆异黄酮，是一种多靶点酪氨酸激酶抑制剂。Genistein 具有抗肿瘤、抗氧化和驱虫作用，还在体内产生类似于雌激素的作用。

Urolithin A 属于天然产物，是一种鞣花酸代谢产物，可以抑制 DNA 合成，诱导细胞凋亡和自噬。Urolithin A 具有抗氧化、抗炎和抗肿瘤活性。

Ethambutol（乙胺丁醇）是可口服的抗结核病药物，也可能够干扰阿拉伯半乳聚糖（arabinogalactan）从而抑制细胞壁合成并抑菌，还可以用于高尿酸血症和视神经病变的动物建模。

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) 是一种P-糖蛋白抑制剂，Ki 值为 59 nM。

AG14361 是一种 PARP-1抑制剂，Ki 值小于 5 nM，在通透的 SW620 细胞和完整的 SW620 细胞中，抑制 PARP-1的活性，IC50值分别为 29 和 14 nM。

Compound 1T-0216 是AKT1-FAK 相互作用的阻滞剂，在不影响基础FAK 磷酸化的情况下，减少对人类SW620结肠癌细胞细胞外压力的FAK 磷酸化的刺激。

PROTAC K-Ras Degrader-3（化合物 40）为特定靶向K-Ras的PROTAC降解剂，其在SW620 KRAS G12D 细胞上体现出极高效力，DC50 值不超过1 nM，同时对SW620 3D 细胞生长的GI50 值亦不高于10 nM。该化合物常用于癌症领域的研究工作。

KRAS inhibitor-37（compound 2）是一种高效KRAS抑制剂，对于KRAS野生型以及其突变体KRAS G12D、KRAS G12C、KRAS G12V的KD值分别为0.004 nM、0.041 nM、0.019 nM和0.144 nM。此外，KRAS inhibitor-37能有效抑制细胞增殖，对H358、SW620、PANC08.13细胞系的IC50范围从<2 nM 至14 nM。因此，该化合物在癌症治疗领域展现出显著的应用潜力。

PROTAC K-Ras degrader-2 (compound 48) 是一种广谱KRAS突变体PROTAC降解剂，对KRAS G12V RAF1的IC50≤200 nM。该化合物可以降解SW620 KRAS G12D，DC50≤200 nM，并抑制SW620 3D细胞扩增，其IC50≤20 nM。

KRAS inhibitor-27 (Compound 15h) 是一种KRAS抑制剂。它对KRAS G12D G12V突变细胞（如AsPC-1和SW620）和KRAS野生型细胞（HT-29）具有抑制作用，其IC50分别为378 nM、0.6 nM和3230 nM。KRAS inhibitor-27还能抑制ERK磷酸化（在AsPC-1和SW620细胞中的IC50分别为0.6 nM和1 nM），并降低DUSP4的表达，从而抑制MAPK信号通路。

TT-232 TFA（147159-51-1 free base）诱导人结肠肿瘤细胞系 SW620 中磷酸酪氨酸磷酸酶活性的双相激活。

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)

Amycolatopsin B is a bacterial metabolite originally isolated fromAmycolatopsisthat has anticancer activity.1It is cytotoxic to NCI H460 lung and SW620 colon cancer cells (IC50s = 0.28 and 0.14 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)

Amycolatopsin C is a polyketide macrolide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 2.7 and 5.7 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin C is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 10 and 5.9 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)

CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg. 1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020)

AMPC 是一种 TFF3 抑制剂，具有抗肿瘤活性，抑制体内肿瘤生长。AMPC 在 TFF3 阳性的 CMS4 结直肠癌细胞中，抑制细胞增殖和存活，可用于研究结直肠癌。