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21

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40253	3-Phenylpropyl isothiocyanate	Others	Others
	3-Phenylpropyl isothiocyanate exhibits a potent inhibitory effect on N-nitrosomethyl-benzylamine (NMBA) tumorigenesis, thereby displaying strong chemopreventive properties [1] [2].
T7955	EB-3D	Apoptosis; AMPK; AChR	Apoptosis; Chromatin/Epigenetic; Neuroscience; PI3K/Akt/mTOR signaling
	EB-3D 是一种选择性胆碱激酶 α 抑制剂，对 ChoKα1 的IC50值为 1 μM。它影响 ChoKα 表达、AMPK 激活、细胞凋亡、内质网应激和脂质代谢，具有抗癌活性。
T9061	EN4 EN4 MYC inhibitor	c-Myc	Cell Cycle/Checkpoint
	EN4 (EN4 MYC inhibitor) 是一种靶向 MYC 的半胱氨酸 171 (C171) 的共价配体。它抑制 MYC 转录活性，下调 MYC 靶标，并具有抗肿瘤作用。它对 c-MYC 的选择性高于 N-MYC 和 L-MYC。
T1167	Cyproterone acetate Androcur,醋酸环丙氯地孕酮,Cyproterone 17-O-acetate,醋酸环丙孕酮	Androgen Receptor	Endocrinology/Hormones
	Cyproterone acetate (Cyproterone 17-O-acetate) 是能够抗雄激素(IC50=7.1 nM) 和孕激素合成的类固醇。它与 progesteron 和糖皮质激素受体有亲和力。
T8350	TPCK	Proteasome	Proteases/Proteasome; Ubiquitination
	TPCK 是丝氨酸蛋白酶抑制剂，通过与 HPV-18 E7 蛋白的视网膜母细胞瘤蛋白 (RB) 结合核心发生反应，并能够消除其 RB 结合能力。将它添加到培养基内，可修饰活角质形成细胞中的 E7 蛋白。
T6322	Copanlisib BAY 80-6946,可泮利塞,库潘尼西	Apoptosis; PI3K	Apoptosis; PI3K/Akt/mTOR signaling
	Copanlisib (BAY 80-6946) 是一种选择性的和 ATP 竞争性的泛 I 类PI3K 抑制剂，具有抗肿瘤活性，对PI3Kα，PI3Kδ，PI3Kβ和PI3Kγ的IC50分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。
T29669	ADP-Ribosylarginine alpha-ADP-ribosylarginine
	ADP-Ribosylarginine can regulate cell proliferation and tumorigenesis.
T10060L	DT-061	Phosphatase	Metabolism
	DT-061 is an orally bioavailable protein phosphatase 2A (PP2A) activator. It could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
T71486	NS-0011
	NS-0011 is an inhibitor of CDK5 translocation which increases CDK5 accumulation in the nucleus, suppressing both cancer cell proliferation and xenograft tumorigenesis.
T9586	Broparestrol (E)-	Others	Others
	Broparestrol (E)- 具有抗生育活性，是啮齿动物乳腺肿瘤发生的有效抑制剂。
T68755	NZ-28
	NZ28, also known as NSC134754, is potent HSF1 inhibitor, which induced inhibition of HSF1, SP1 and NF-κB triggers the loss of the natural killer cell-activating ligands MICA/B on human tumor cells. Heat-shock transcription factor HSF1 has a critical role in human epidermal growth factor receptor-2-induced cellular transformation and tumorigenesis.
T79763	UNC9512	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	UNC9512是一种针对甲基赖氨酸读取器p53结合蛋白1 (53BP1) 的有效拮抗剂, 适用于探究53BP1在DNA修复、基因编辑及肿瘤发生等生物学过程的功能。
T62694	(S)-GFB-12811
	(S)-GFB-12811 (compound 596) 是一种选择性的、选择性的 CDK5 抑制剂 (IC50<10 nM)。(S)-GFB-12811 能够用于细胞周期进程、神经元发育、肿瘤发生的研究。
T82165	HTH-02-006	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	HTH-02-006，一种NUAK2抑制剂（IC50 = 126 nM），能够降低HuCCT-1细胞中磷酸化MYPT1水平，并抑制YAP驱动的细胞增殖、肝肿大和肿瘤发生，同时具备抗纤维化保护效果。
T82762	Cdc25A (80-93) (human)
	Cdc25A (80-93) (human)为调控细胞周期蛋白D1及G1/S转换中相关蛋白表达，进而控制细胞增殖与肿瘤发生的多肽。该化合物在癌症研究中具应用价值。
T74602	PROTAC EZH2 Degrader-1
	PROTACEZH2 Degrader-1 (Compound 150d)是高效的PROTACEZH2降解剂，能够抑制EZH2甲基转移酶的活性，其IC50值为2.7 nM。由于EZH2在许多肿瘤的发生及进展中具有关键作用，这种化合物的研发具有重要意义。
T71188	LY2780301
	LY2780301 is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor LY2780301 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway, thereby leading to inhibition of cell proliferation and the induction of apoptosis in tumor cells. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signa...
T71267	GNF-8625
	GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in vivo antitumor efficacy when administered at ascending doses twice daily (bid) for 14 days in rats. Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer type...
T76791	Seribantumab
	Seribantumab (MM 121) 是一种完全人 IgG2单克隆抗体，靶向 HER3。Seribantumab 阻断 ErbB 家族成员及其下游信号的激活。Seribantumab 在体内、外抑制乳腺癌、肺癌和卵巢癌患者源性癌症模型中神经调节蛋白 (NRG1) 融合依赖的肿瘤发生。
T35778	Ochratoxin A-13C20 Ochratoxin A-13C20
	Ochratoxin A-13C20is intended for use as an internal standard for the quantification of ochratoxin A by GC- or LC-MS. Ochratoxin A is a mycotoxin that has been found inAspergillusandPenicillium.1It increases lipid peroxide levels and the number of apoptotic cells, as well as reduces superoxide dismutase activity in rat kidney when administered at a dose of 120 μg/kg.2Topical application of ochratoxin A (80 μg/mouse) induces DNA damage, cell cycle arrest at the G0/G1phase, and apoptosis in mouse ...
T76120	Phospholipase D
	PhospholipaseD (PLD) ，即磷脂酶 D，是磷脂酶超家族的一种酶，广泛存在于细菌、酵母、植物、动物和病毒中，常用于生化研究。PhospholipaseD 可以催化甘油磷脂的磷酸二酯键水解，产生磷脂酸和可溶性胆碱。PhospholipaseD 参与了多种疾病相关过程，包括糖尿病、动脉粥样硬化形成、肥胖、肿瘤发生、免疫反应和神经内分泌功能。

化合物

3-Phenylpropyl isothiocyanate

Cat.No: T40253

Target: Others

Cat.No: T7955

Target: Apoptosis, AMPK, AChR

Cat.No: T9061

Synonym: EN4 MYC inhibitor

Target: c-Myc

Cyproterone acetate

Cat.No: T1167

Synonym: Androcur,醋酸环丙氯地孕酮,Cyproterone 17-O-acetate,醋酸环丙孕酮

Target: Androgen Receptor

Cat.No: T8350

Target: Proteasome

Cat.No: T6322

Synonym: BAY 80-6946,可泮利塞,库潘尼西

Target: Apoptosis, PI3K

ADP-Ribosylarginine

Cat.No: T29669

Synonym: alpha-ADP-ribosylarginine

Cat.No: T10060L

Target: Phosphatase

Cat.No: T71486

Broparestrol (E)-

Cat.No: T9586

Target: Others

Cat.No: T68755

Cat.No: T79763

Target: DNA/RNA Synthesis

Cat.No: T62694

Cat.No: T82165

Target: AMPK

Cdc25A (80-93) (human)

Cat.No: T82762

PROTAC EZH2 Degrader-1

Cat.No: T74602

Cat.No: T71188

Cat.No: T71267

Cat.No: T76791

Ochratoxin A-13C20

Cat.No: T35778

Synonym: Ochratoxin A-13C20

Phospholipase D

Cat.No: T76120

Cat. No.	Product Name	Target	Signaling Pathways
T3055	Liensinine Perchlorate	Apoptosis; Others	Apoptosis; Others
	Liensinine Perchlorate 是元莲的成分，可诱导结直肠癌细胞凋亡，具有抗高血压和抗癌活性。
T8017	2-Undecanone Methylnonylketone,甲基壬基甲酮	Others	Others
	2-Undecanone (Methylnonylketone) 能够抑制 DnaKJE-ClpB 双酮依赖的热灭活细菌萤光素酶重折叠。它对肺肿瘤发生具有抑制作用。
T1051	Retinoic acid 维生素A酸,Vitamin A acid,ATRA,all-trans-Retinoic acid,Tretinoin	Retinoid Receptor; Endogenous Metabolite; PPAR; Autophagy	Autophagy; DNA Damage/DNA Repair; Metabolism
	Retinoic acid (Tretinoin) 是维生素 A 的代谢产物，是一种视黄酸受体 RAR 的天然激动剂，抑制 RARα/β/γ (IC50=14 nM)。Retinoic acid 可以诱导细胞分化、减少细胞增殖和抑制肿瘤发生。
T2915	Bardoxolone RTA 401,齐墩果烷三萜化合物,CDDO	Others; Nrf2	Immunology/Inflammation; Others
	Bardoxolone (CDDO) 是新型核调节因子激活剂。
T14317	ar-Turmerone (+)-ar-Turmerone	Others	Others
	ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation.
TN5153	Torilin	MMP; ERK; IκB/IKK; p38 MAPK; NF-κB; Tyrosinase; Reductase; DNA/RNA Synthesis; JNK	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Endocrinology/Hormones; MAPK; Metabolism; NF-κB; Proteases/Proteasome
	Torilin 是一种睾酮5α还原酶抑制剂，它（IC50=31.7+/-4.23μM）对5α还原酶的抑制作用强于α-亚麻酸（IC50=160.3+/-24.62μM），但弱于非那雄胺（IC50=0.38+/-0.06μM）。Torilin 具有免疫调节、肝脏保护和抗炎特性，它通过限制 TAK1介导的 MAP 激酶和 NF-βB 活化来抑制炎症，它可以减轻关节炎的严重程度，改变 dLN 或关节中的白细胞活化，并恢复血清和脾细胞细胞因子失衡。托利林抑制α-黑素细胞刺激激素激活的 B16黑色素瘤细胞中的黑色素生成，IC（50）值为25μM。Torilin 对枯草芽孢杆菌 ATCC 6633孢子和营养细胞表现出优异的抗菌活性。Torilin 在体内和体外都具有强大的抗血管生成活性，它可能通过抑制肿瘤侵袭来抑制肿瘤发生，逆转癌细胞的多药耐药性，它可以增强阿霉素、长春碱、紫杉醇和秋水仙碱对多药耐药 KB-V1和 MCF7/ADR 细胞的细胞毒性。

天然产物

Liensinine Perchlorate

Cat.No: T3055

Target: Apoptosis, Others

Cat.No: T8017

Synonym: Methylnonylketone,甲基壬基甲酮

Target: Others

Cat.No: T1051

Synonym: 维生素A酸,Vitamin A acid,ATRA,all-trans-Retinoic acid,Tretinoin

Target: Retinoid Receptor, Endogenous Metabolite, PPAR, Autophagy

Cat.No: T2915

Synonym: RTA 401,齐墩果烷三萜化合物,CDDO

Target: Others, Nrf2

Cat.No: T14317

Synonym: (+)-ar-Turmerone

Target: Others

Cat.No: TN5153

Target: MMP, ERK, IκB/IKK, p38 MAPK, NF-κB, Tyrosinase, Reductase, DNA/RNA Synthesis, JNK

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