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18

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11631	iFSP1	Ferroptosis	Apoptosis
	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。
T21331	SAR-020106	Chk	Cell Cycle/Checkpoint
	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。
T5858	Sertindole Lu 23-174,舍吲哚	Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy	Autophagy; GPCR/G Protein; Neuroscience
	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。
T23479L	TT-232 TFA（147159-51-1 free base）	Others	Others
	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。
T9544	Compound 1T-0216	Others	Others
	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。
T9545	Compound 1T-0219 (SC)	FAK	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Compound 1T-0219 (SC) 是一种 AKT1-FAK 相互作用的阻断剂，可减少对人 SW620 结肠癌细胞中细胞外压力的 FAK 磷酸化的刺激，而不影响基础 FAK 磷酸化。
T6339	AG14361 AG 14361,AG-14361	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	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。
T72576	Transketolase-IN-4	Antibacterial	Microbiology/Virology
	Transketolase-IN-4 是一种转酮酶抑制剂，IC50值为3.9 μM。Transketolase-IN-4 对结核分枝杆菌 DXS 有抑制作用，IC50 为 114.1 μM。 Transketolase-IN-4 抑制 SW620、LS174T 和 MIA PaCa-2 的肿瘤细胞增殖。
T69976	WS-691
	WS-691 is a highly Potent and Orally Active ABCB1 Modulator. WS-691 significantly increased sensitization of ABCB1-overexpressed SW620/Ad300 cells to paclitaxel (PTX) (IC50 = 22.02 nM). WS-691 significantly increased the intracellular concentration of PTX and [3H]-PTX while decreasing the efflux of [3H]- PTX in SW620/Ad300 cells by inhibiting the efflux function of ABCB1. WS-691 could stabilize ABCB1 by directly binding to ABCB1 WS-691 increased the sensitivity of SW620/Ad300 cells to PTX in vi...
T37540	Amycolatopsin B
	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)
T37539	Amycolatopsin A
	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: Antimycobacteria...
T64016	WS-898
	WS-898 是 ABCB1 的高效抑制剂，能够逆转耐药SW620/Ad300、KB-C2 和 HEK293/ABCB1 细胞对紫杉醇（PTX）的耐药性，他们的 IC50 值分别为 5.0、3.67 和 3.68 nM。
T79685	PI3Kα-IN-13	PI3K	PI3K/Akt/mTOR signaling
	PI3Kα-IN-13（Compound 18a）是一款高效的PI3Kα抑制剂，具有2.5 nM的IC50值。此化合物能够诱发肿瘤细胞的凋亡，并显著抑制癌细胞的增殖，具体IC50值为MCF-7细胞系0.75 μM、HCT-116细胞系3.79 μM、MDA-MB-231细胞系13.71 μM和SW620细胞系9.85 μM。此外，PI3Kα-IN-13能有效阻止肿瘤细胞集落的形成、迁移以及侵袭。
T37541	Amycolatopsin C
	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 ...
T60793	Tubulin inhibitor 26
	Tubulin inhibitor 26 (compound 3c) 是一种吲唑衍生物，是微管蛋白抑制剂，对 HepG2、HCT116、SW620、HT29 和 A549 癌细胞系具有显著的低纳摩尔效力。Tubulin inhibitor 26 抑制G2/M 期肿瘤细胞，并且诱导细胞凋亡。Tubulin inhibitor 26 在体内抑制肿瘤生长，并且不影响小鼠体重。
T37006	Previridicatumtoxin
	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 μ...
T38381	CAY17c
	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,...
T65994	(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
	Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation...

化合物

Cat.No: T11631

Target: Ferroptosis

Cat.No: T21331

Target: Chk

Cat.No: T5858

Synonym: Lu 23-174,舍吲哚

Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Autophagy

TT-232 TFA（147159-51-1 free base）

Cat.No: T23479L

Target: Others

Compound 1T-0216

Cat.No: T9544

Target: Others

Compound 1T-0219 (SC)

Cat.No: T9545

Target: FAK

Cat.No: T6339

Synonym: AG 14361,AG-14361

Target: PARP

Transketolase-IN-4

Cat.No: T72576

Target: Antibacterial

Cat.No: T69976

Amycolatopsin B

Cat.No: T37540

Amycolatopsin A

Cat.No: T37539

Cat.No: T64016

Cat.No: T79685

Target: PI3K

Amycolatopsin C

Cat.No: T37541

Tubulin inhibitor 26

Cat.No: T60793

Previridicatumtoxin

Cat.No: T37006

Cat.No: T38381

(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide

Cat.No: T65994

Cat. No.	Product Name	Target	Signaling Pathways
T2763	Panaxadiol 人参二醇,20(R)-Panaxadiol	Others; HIF/HIF Prolyl-Hydroxylase	Chromatin/Epigenetic; Metabolism; Others
	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。
TN5422	Ciwujiatone
	Ciwujiatone exhibits significant activities against colon cancer cell lines SW480 and SW620.
TN1865	Licoricesaponin A3 甘草皂苷A3	Others	Others
	Licoricesaponin A3 shows the cytotoxic activity against the human cancer cell lines MGC-803, SW620, and SMMC-7721 with IC50 > 100 μMol/L.
TN5204	Uralsaponin C	Others	Others
	Uralsaponin C shows the cytotoxic activity against the human cancer cell lines MGC-803, SW620, and SMMC-7721 with IC50 > 100 μmol/L.
TN3152	6-Acetonyldihydrochelerythrine	ERK; BCL; Akt; HIV Protease; PPAR; p53	Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	6-Acetonyldihydrochelerythrine exhibits significant antioxidant activities, it exhibits significant anti-HIV activity in H9 lymphocytes with EC50 and TI (Therapeutic Index) values of 1.77 microg/mL and 14.6, respectively. 6-Acetonyldihydrochelerythrine is
TN4046	Excisanin A	MMP; FAK; PARP; GSK-3; NF-κB; Wnt/beta-catenin; Akt; Caspase; PI3K; Prostaglandin Receptor; JNK	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; MAPK; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors
	ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the ...

天然产物

Cat.No: T2763

Synonym: 人参二醇,20(R)-Panaxadiol

Target: Others, HIF/HIF Prolyl-Hydroxylase

Cat.No: TN5422

Licoricesaponin A3

Cat.No: TN1865

Synonym: 甘草皂苷A3

Target: Others

Cat.No: TN5204

Target: Others

6-Acetonyldihydrochelerythrine

Cat.No: TN3152

Target: ERK, BCL, Akt, HIV Protease, PPAR, p53

Cat.No: TN4046

Target: MMP, FAK, PARP, GSK-3, NF-κB, Wnt/beta-catenin, Akt, Caspase, PI3K, Prostaglandin Receptor, JNK

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