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32

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T10342	Antitumor agent-2	Others	Others
	Antitumor agent-2 具有抗炎和抗肿瘤活性，可用于研究癌症。
TPL0265	4-(Benzo[d]oxazol-2-yl)aniline
	4-(Benzo[d]oxazol-2-yl)aniline 是一种有效的抗肿瘤剂，对乳腺癌细胞系具有抑制活性。
T3459	VK3-OCH3 2-[(2-Methoxy)ethylthio]-3-methyl-1,4-na	Others	Others
	VK3-OCH3 (2-[(2-Methoxy)ethylthio]-3-methyl-1,4-na) 是一种通过血红素加氧酶(HO-1) 相关机制的选择性抗肿瘤剂；维生素 K3 类似物。
T3166	VX-11e Vertex-11e,VTX-11e,TCS ERK 11e	ERK; GSK-3; FLT; CDK; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	VX-11e (TCS ERK 11e) 是可口服的ERK 高效选择性抑制剂，Ki 值小于 2 nM。
TNU0168	2'-Deoxy-2'-fluoro-beta-D-arabinoguanosine	Apoptosis	Apoptosis
	Nucleoside Derivatives - Fluoro-modified nucleosides, Arabino-nucleosides, 2’-Modified nucleosides; Drugs and Inhibitors; Anticancer agent; Impurity C of Clofarabine
T11718	JI051 JI-051	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	JI051 具有抗肿瘤作用，能够与癌症相关蛋白伴侣 prohibitin 2 (PHB2) 相互作用，通过抑制 Notch 下游效应基因 Hes1 转录来促使细胞周期停滞，抑制HEK293 细胞和胰腺癌细胞增殖。
T62814	Antitumor agent-77
	Antitumor agent-77 对癌细胞的生长和迁移具有抑制作用，具有抗癌作用。Antitumor agent-77 能够抑制 GPx-4 和提高 COX2 引发铁下垂。Antitumor agent-77 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，阻碍肿瘤细胞上皮间质转化 (EMT) 过程。
T63768	Antitumor agent-78
	Antitumor agent-78 能够抑制 GPx-4 和升高 COX2 ，进而导致铁下垂 (ferroptosis)。Antitumor agent-78 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，抑制肿瘤细胞上皮间质转化 (EMT) 过程。Antitumor agent-78 表现出抗肿瘤效果，并能够抑制癌细胞的生长和迁移。
T64022	Antitumor agent-37
	Antitumor agent-37 表现出有效的抗增殖和抗转移效果。Antitumor agent-37 能够诱导严重的 DNA 损伤，进而导致 γ-H2AX 和 p53 的高表达。Antitumor agent-37 可利用线粒体凋亡通路 Bcl-2/Bax/caspase3，诱导肿瘤细胞凋亡 (apoptosis)。Antitumor agent-37 可以抑制 PD-L1 的表达，提高肿瘤组织中 CD3+ 和 CD8+ T 浸润细胞，明显改善免疫反应。
T14879	CB 300919	Others	Others
	CB 300919 is a quinazoline-based antitumor agent with high activity in the CH1 human ovarian tumor xenograft and has continuous exposure (96 h) growth inhibition (IC50: 2 nM).
T28411	Physapubenolide NSC 368674,NSC368674,NSC-368674
	Physapubenolide is natural cytotoxic withanolide antitumor agent. Physapubenolide induces apoptosis by decreasing mitochondrial membrane potential and elevating the Bax/Bcl-2 protein expression ratio.
T15180	Duocarmycin A	Caspase	Apoptosis; Proteases/Proteasome
	Duocarmycin A, an antitumor antibiotic, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results in HLC-2 cells typically apoptotic changes.
T63523	Duocarmycin analog-2
	Duocarmycin analog-2 是有效的 DNA 烷基化剂，表现出抗肿瘤作用，能够用于免疫偶联物的合成。
T12925	Sitravatinib malate MGCD516 malate,MG-516 malate	TAM Receptor	Tyrosine Kinase/Adaptors
	Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
T61996	Antiproliferative agent-6
	Antiproliferative agent-6 (compound 8a) 是有效的抗肿瘤化合物。Antiproliferative agent-6 具有抗增殖活性，抑制癌细胞系 HCT116、MCF-7、H460 和非肿瘤非整倍体永生角质细胞 HaCaT 的 GI50分别为 0.5 μM、2 μM、0.7 μM 和 3.5 μM。
T75667	Neamine
	Neamine，新霉素降解产物，为广谱氨基糖苷类抗生素。作为抗血管生成剂，针对血管生成素 (angiogenin)，展现抗菌、抗肿瘤及神经保护活性。
T83008	Antitumor agent-119
	Antitumor agent-119（化合物13K）为2-苯并恶唑基腙衍生物，显示抗癌活性。该化合物对Butkitt、CCRF-CEM、HeLa和HT-29细胞系展现出细胞生长抑制作用，其IC50值分别为30 nM、140 nM、100 nM和40 nM。
T81835	MC-betaglucuronide-MMAE-2
	MC-betaglucuronide-MMAE-2 是由微管蛋白聚合抑制剂 MMAE 与 ADC linker MC-betaglucuronide 可降解连接组成的抗体-活性分子偶联物部分。
T74393	Antitumor agent-36
	Antitumor agent-36 具有有效的抗增殖和抗转移活性，能诱导严重的 DNA 损伤，并通过增加 γ-H2AX 和 p53 的表达促进肿瘤细胞通过 Bcl-2/Bax/caspase3 线粒体凋亡通路的 (apoptosis)。此外，Antitumor agent-36 还能通过抑制 PD-L1 的表达显著增加肿瘤组织中 CD3+ 和 CD8+ T 浸润细胞，从而改善免疫反应。
T79111	PI3Kγ inhibitor 7	PI3K	PI3K/Akt/mTOR signaling
	PI3Kγ inhibitor7（compound 2）作为一种有效的PI3Kγ抑制剂，拥有口服活性，并对PI3Kα、PI3Kβ、PI3Kγ、PI3Kδ的抑制作用，其IC50值分别为4768 nM、878.1 nM、3.42 nM、355.2 nM。此外，PI3Kγ inhibitor7还展现出了抗肿瘤活性。
T76940	Cantuzumab ravtansine
	Cantuzumab ravtansine (IMGN242; huC242-DM4) 是一种 ADC，由一种人源化单克隆抗体 huC242，通过二硫键与 DM4 (DM4) 共价连接。Cantuzumab ravtansine 对一系列 CanAg 阳性人肿瘤异种移植物具有广泛的抗肿瘤功效。
T9684	(Z)-Orantinib
	(Z)-Orantinib ((Z)-SU6668) 是一种有效，选择性，具有口服活性和 ATP 竞争性的 Flk‐1/KDR，PDGFRβ和 FGFR1抑制剂，IC50值分别为 2.1，0.008 和 1.2 μM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂，可诱导已形成的肿瘤消退。
T35645	4-oxo Cyclophosphamide
	4-oxo Cyclophosphamide is an inactive metabolite of the alkylating agent cyclophosphamide .1,2It is formed from cyclophosphamide through a 4-hydroxycyclophosphamide intermediate by aldehyde dehydrogenases.2 1.Struck, R.F., Kirk, M.C., Mellett, L.B., et al.Urinary metabolites of the antitumor agent cyclophosphamideMol. Pharmacol.7(5)519-529(1971) 2.de Jonge, M.E., Huitema, A.D.R., Rodenhuis, S., et al.Clinical pharmacokinetics of cyclophosphamideClin. Pharmacokinet.44(11)1135-1164(2005)
T62479	3CPLro-IN-1
	3CPLro-IN-1 (compound A17) 是一种有效的、口服具有活力的 SARS-CoV-2 3CLpro 抑制剂 (IC50: 5.65 μM)。3-糜蛋白酶样半胱氨酸蛋白酶 (3CLpro) 是一种病毒复制中不可或缺的蛋白质，是一种有吸引力的、对抗 COVID-19 的药物靶点。
T68400	STA-9584
	STA-9584 is a potent vascular disrupting agent, which exhibits potent antitumor activity by selectively targeting microvasculature at both the center and periphery of tumors. In vitro, 2-methoxy-5-(5-(3,4,5-trimethoxyphenyl)isoxazol-4-yl)aniline (STA-9122) (active metabolite of STA-9584 ) displayed increased potency relative to other tubulin-binding agents and was highly cytotoxic to tumor cells. STA-9584 induced significant tumor regressions in prostate and breast xenograft models in vivo and, ...
T60704	Loxoprofen sodium (dihydrate)
	Loxoprofen sodium dihydrate 是一种非甾体类口服抗炎药，具有镇痛和解热作用。Loxoprofen sodium dihydrate 显示出抗肿瘤活性，并且可减少动脉粥样硬化。Loxoprofen sodium dihydrate 是COX 的非选择性抑制剂，对 COX-1 和 COX-2 的IC50值分别为 6.5 和 13.5 μM。
T80523	Azurin p28 peptide
	Azurin p28 peptide是一种具有肿瘤穿透能力和抗肿瘤活性的肽。它通过与p53结合形成p28:p53复合物，从而降低p53在蛋白酶体中的降解，进而诱导细胞凋亡(apoptosis)或使细胞周期停滞。此外，Azurin p28 peptide通过抑制VEGFR-2、FAK和Akt的磷酸化表现出抗血管生成效果，抑制p53阳性肿瘤的生长。
T36745	cDPCP
	cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when ad...
T74546	FAP-2286
	FAP-2286，一种与放射性核素螯合剂 DOTA 偶联的 FAP 结合肽大环化合物。FAP-2286 对人 FAP 蛋白具有强亲和力，Kd 为 1.1 nM。FAP-2286 具有抗肿瘤活性。FAP-2286 可用放射性核素标记，用于治疗及诊断。
T36967	LSN3106729 hydrochloride
	LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods o...
T63769	EGFR-IN-60
	EGFR-IN-60 是一种有效的、口服具有活力的、安全的抗肿瘤剂。EGFR-IN-60 能够明显抑制 EGFRWT (IC50: 83 nM)、EGFRT790M (IC50: 26 nM)、EGFRL858R (IC50: 53 nM) 和 JAK3 (IC50: 69 nM)。EGFR-IN-60 能够抑制携带 EGFRT790M 突变的 H1975 细胞 (IC50: 1.32 μM) ，并抑制过表达 EGFRWT 的 A431 细胞 (IC50: 4.96 μM)。EGFR-IN-60 能够提高 Bax/Bcl-2 比率，进而诱导细胞凋亡诱导并导致细胞死亡。
T71261	Arsthinol
	Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50/IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 +/- 0.08 micromol/l after 24 h) than As(2)O(3) (IC50 = 1.60 +/- 0.23 micro...

化合物

Antitumor agent-2

Cat.No: T10342

Target: Others

4-(Benzo[d]oxazol-2-yl)aniline

Cat.No: TPL0265

Cat.No: T3459

Synonym: 2-[(2-Methoxy)ethylthio]-3-methyl-1,4-na

Target: Others

Cat.No: T3166

Synonym: Vertex-11e,VTX-11e,TCS ERK 11e

Target: ERK, GSK-3, FLT, CDK, Aurora Kinase

2'-Deoxy-2'-fluoro-beta-D-arabinoguanosine

Cat.No: TNU0168

Target: Apoptosis

Cat.No: T11718

Synonym: JI-051

Target: Gamma-secretase

Antitumor agent-77

Cat.No: T62814

Antitumor agent-78

Cat.No: T63768

Antitumor agent-37

Cat.No: T64022

Cat.No: T14879

Target: Others

Physapubenolide

Cat.No: T28411

Synonym: NSC 368674,NSC368674,NSC-368674

Cat.No: T15180

Target: Caspase

Duocarmycin analog-2

Cat.No: T63523

Sitravatinib malate

Cat.No: T12925

Synonym: MGCD516 malate,MG-516 malate

Target: TAM Receptor

Antiproliferative agent-6

Cat.No: T61996

Cat.No: T75667

Antitumor agent-119

Cat.No: T83008

MC-betaglucuronide-MMAE-2

Cat.No: T81835

Antitumor agent-36

Cat.No: T74393

PI3Kγ inhibitor 7

Cat.No: T79111

Target: PI3K

Cantuzumab ravtansine

Cat.No: T76940

Cat.No: T9684

4-oxo Cyclophosphamide

Cat.No: T35645

Cat.No: T62479

Cat.No: T68400

Loxoprofen sodium (dihydrate)

Cat.No: T60704

Azurin p28 peptide

Cat.No: T80523

Cat.No: T36745

Cat.No: T74546

LSN3106729 hydrochloride

Cat.No: T36967

Cat.No: T63769

Cat.No: T71261

Cat. No.	Product Name	Target	Signaling Pathways
T1257	Bestatin Ubenimex,乌苯美司	Others; Aminopeptidase; Antibacterial; Antibiotic; LTR	Immunology/Inflammation; Metabolism; Microbiology/Virology; Others
	Bestatin (Ubenimex) 是 CD13 (Aminopeptidase N)/APN 和 leukotriene A4 hydrolase 抑制剂，可用于癌症研究。
T75563	Vanicoside E
	Vanicoside E 是一种抗氧化和抗癌剂。Vanicoside E 抑制L-Tyrosine 和L-DOPA，IC50为 45.23 μM 和 189.96 μM。
T14121	Actinonin (-)-Actinonin	Aminopeptidase	Metabolism
	Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM, it also is an apoptosis inducer. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase, it also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
T81170	Shishijimicin A
	Shishijimicin A是一款从子囊菌Didemnum proliferum中分离出的新型抗肿瘤剂，具备突出的细胞毒性及抗肿瘤活性。作为点击化学试剂，Shishijimicin A内含Alkyne基团，能够与含Azide基团的分子通过铜催化的叠氮-炔环加成反应(CuAAc)进行作用。

天然产物

Cat.No: T1257

Synonym: Ubenimex,乌苯美司

Target: Others, Aminopeptidase, Antibacterial, Antibiotic, LTR

Cat.No: T75563

Cat.No: T14121

Synonym: (-)-Actinonin

Target: Aminopeptidase

Shishijimicin A

Cat.No: T81170

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