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21

抑制剂 & 化合物

10

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16850	SB-265610 GSK-CXCR2	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	SB-265610 (GSK-CXCR2) 是竞争性非肽变构CXCR2选择性拮抗剂，可阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性，IC50分别为 3.7 和 70 nM。
T6939	PFI-3 PFI 3	Epigenetic Reader Domain	Chromatin/Epigenetic
	PFI-3是一种选择性，可渗透细胞的SMARCA2/4溴结构域抑制剂，Kd 值为89 nM，可延迟和预防乳腺癌。
T77416	Opicinumab BIIB033	Others	Others
	Opicinumab (BIIB033) 是一种新型抗 LINGO-1 的单克隆抗体，可用于预防和延缓急性视神经炎和复发性多发性硬化。
T61864	Melengestrol acetate	Progesterone Receptor	Others
	Melengestrol acetate 是孕酮的衍生物，充当皮质类固醇激素。 Melengestrol acetate 可以促进月经活动和妊娠维持的子宫内膜增殖延迟。
T1458	Epalrestat ONO2235,依帕斯他,依帕司他	Reductase	Endocrinology/Hormones; Metabolism
	Epalrestat (ONO2235) 是醛糖还原酶抑制剂，在长期治疗中具有良好的耐受性。它可以有效改善糖尿病神经病变的相关症状并延缓疾病的进展，特别是在微血管病变有限且血糖控制良好的患者中。
T10215	AAPK-25	Apoptosis; PLK; Aurora Kinase	Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic
	AAPK-25 是选择性的Aurora/PLK 激酶双重抑制剂，显示出抗肿瘤活性。它可造成有丝分裂延迟并阻滞前中期细胞，通过生物标志物组蛋白 H3Ser10磷酸化反应，导致细胞凋亡激增。
T77697	BML-278 BML278,BML 278	Sirtuin; Histone Methyltransferase	Chromatin/Epigenetic; DNA Damage/DNA Repair
	BML-278 是一种 SIRT1 激活剂，EC150 值为 1 μM。BML-278 增加父本和母本原核中的 H3K9 甲基化并抑制 H3K9 乙酰化，可用于改善早期胚胎发育。BML-278 促使原代人间充质细胞的细胞周期停止在 G1/S 期，可用于延缓衰老。BML-278 减少 U937 细胞中的微管蛋白乙酰化，增加小鼠 C2C12 成肌细胞的线粒体密度。
T2170	SKF-96365 hydrochloride 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑,SKF96365	Apoptosis; Potassium Channel; Calcium Channel; TRP/TRPV Channel; Autophagy	Apoptosis; Autophagy; Membrane transporter/Ion channel; Metabolism
	SKF-96365 hydrochloride (SKF96365) 是store-operated Ca2+entry 抑制剂，也是TRP channel 阻滞剂。它显著抑制豚鼠离体心脏 hERG、hKCNQ1/hKCNE1、hKir2.1 和 hKv4.3 电流，延长QTc 间期。它通过诱导结直肠癌细胞的细胞周期阻滞和凋亡起抗肿瘤作用。
T31280	Decaborane, ethyl-, Ethyldecaborane,Decaborane, ethyl-,Ethyldekaboran
	Decaborane, ethyl-, Nonaborane and decaborane cluster anions can enhance the ignition delay in hypergolic ionic liquids and induce hypergolicity in molecular solvents.
T73413	Cadein1
	Cadein1 是一种异喹啉衍生物，在p53功能缺失的癌细胞中，可导致 G2/M 延迟和caspase 依赖的凋亡。
T21921	Valeroyl Salicylate 2-Valeryloxybenzoic acid,戊酰基水杨酸	Others	Others
	Valeroyl Salicylate (2-Valeryloxybenzoic acid) 具有抗炎作用，可延长寿命，延缓随年龄增长而导致的自发活动下降，并提高抗压能力。
T69380	Cinnamic acid, hydrazide
	Cinnamic acid, hydrazide is an unsaturated carboxylic acid and precursor to aspartame via enzyme-catalysed amination to phenylalanine. Cinnamic acid may be useful in prevention or treatment of Diabetes through various mechanism of actions including stimulation of insulin secretion, improvement of pancreatic β-cell functionality, inhibition of hepatic gluconeogenesis, enhanced glucose uptake, increased insulin signaling pathway, delay of carbohydrate digestion and glucose absorption, and inhibiti...
T77141	Pegaldesleukin
	Pegaldesleukin 是一种聚乙二醇与白细胞介素-2 的偶联物 (PEG-IL2)。Pegaldesleukin 具有抗病毒活性，在 HIV 中有潜在应用，可能通过保留免疫组库来延缓 HIV 感染的进展。
T69821	AMP423
	AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226/S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T/C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive.
T32026	GYKI-13324 GYKI 13324,GYKI13324
	GYKI-13324 is bifunctional nitrosoureido derivative and alkylating agent. GYKI-13324 was studied on human colorectal tumor xenograft lines. Given orally in single or multiple daily doses, GYKI-13324 produced long-term or total regression of adenomatous, b
T71206	Tiagabine-d6 hydrochloride
	Tiagabine-d6 is intended for use as an internal standard for the quantification of tiagabine by GC- or LC-MS. Tiagabine is an inhibitor of GABA transporter 1. It inhibits seizures induced by DMCM in mice. Tiagabine reduces allodynia in a rodent model of neuropathic pain when used at a dose of 72.8 µmol/kg, and it acts synergistically with gabapentin to delay pain responses in mice in the hot plate test. Formulations containing tiagabine have been used as adjunctive therapies in the treatment of ...
T68861	MS-0022
	MS-0022 is a SMO antagonist. MS-0022 showed effective Hh signaling pathway inhibition at the level of SMO in the low nM range, and Hh pathway inhibition downstream of Suppressor of fused (SUFU) in the low µM range. MS-0022 reduced growth in the tumor cell lines PANC-1, SUIT-2, PC-3 and FEMX in vitro. MS-0022 is a treatment led to a transient delay of tumor growth that correlated with a reduction of stromal Gli1 levels in SUIT-2 xenografts in vivo.
T60602	hCAIX/XII-IN-5
	hCAIX/XII-IN-5 (Coumarin 9a) 是一种碳酸酐酶 (CA) 抑制剂，具有出色的 hCA IX/XII 选择性，对 hCA I 和 hCA II 的Ki 值分别为 93.9 和 85.7 nM。hCAIX/XII-IN-5 对癌细胞具有抗增殖活性，可延迟细胞周期并诱导细胞凋亡。
T70552	Ipatasertib tosylate
	Ipatasertib, also known as GDC0068, is an orally active, potent and selective Akt inhibitor. GDC-0068 blocked Akt signaling both in cultured human cancer cell lines and in tumor xenograft models. Inhibition of Akt activity by GDC-0068 resulted in blockade of cell-cycle progression and reduced viability of cancer cell lines. Markers of Akt activation, including high-basal phospho-Akt levels, PTEN loss, and PIK3CA kinase domain mutations, correlate with sensitivity to GDC-0068. In multiple tumor...
T68480	4SC-207
	4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome a...
T38269	Purfalcamine
	Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras...

化合物

Cat.No: T16850

Synonym: GSK-CXCR2

Target: CXCR

Cat.No: T6939

Synonym: PFI 3

Target: Epigenetic Reader Domain

Cat.No: T77416

Synonym: BIIB033

Target: Others

Melengestrol acetate

Cat.No: T61864

Target: Progesterone Receptor

Cat.No: T1458

Synonym: ONO2235,依帕斯他,依帕司他

Target: Reductase

Cat.No: T10215

Target: Apoptosis, PLK, Aurora Kinase

Cat.No: T77697

Synonym: BML278,BML 278

Target: Sirtuin, Histone Methyltransferase

SKF-96365 hydrochloride

Cat.No: T2170

Synonym: 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑,SKF96365

Target: Apoptosis, Potassium Channel, Calcium Channel, TRP/TRPV Channel, Autophagy

Decaborane, ethyl-,

Cat.No: T31280

Synonym: Ethyldecaborane,Decaborane, ethyl-,Ethyldekaboran

Cat.No: T73413

Valeroyl Salicylate

Cat.No: T21921

Synonym: 2-Valeryloxybenzoic acid,戊酰基水杨酸

Target: Others

Cinnamic acid, hydrazide

Cat.No: T69380

Cat.No: T77141

Cat.No: T69821

Cat.No: T32026

Synonym: GYKI 13324,GYKI13324

Tiagabine-d6 hydrochloride

Cat.No: T71206

Cat.No: T68861

Cat.No: T60602

Ipatasertib tosylate

Cat.No: T70552

Cat.No: T68480

Cat.No: T38269

Cat. No.	Product Name	Target	Signaling Pathways
T2S0842	Scutellarin methyl ester Scutellarin methylester,野黄芩苷甲酯	Others	Others
	Scutellarin methyl ester (3-Oxotirucallenoic Acid) 是一种灯盏花素的成分, 其中灯盏花素是灯盏花中几种黄酮类化合物的粗提物。
T5231	2-Methylsuccinic acid Pyrotartaric Acid,Methylbutanedioic acid,甲基丁二酸	Others; Endogenous Metabolite	Metabolism; Others
	2-Methylsuccinic acid (Pyrotartaric Acid) 是乙基丙二酸脑病的主要生化指标，是人体液中的正常代谢物。
T3864	Erianin	BCL; Antibacterial	Apoptosis; Microbiology/Virology
	Erianin 能抑制吲哚胺-2,3-双加氧酶诱导的肿瘤血管生成，可用作退烧药和止疼剂。
TN1594	DL-Syringaresinol (±)-Syringaresinol	Antioxidant; Antifungal	Microbiology/Virology; oxidation-reduction
	DL-Syringaresinol ( (±)-Syringaresinol) 是一种来自与人参浆果的木质素，具有抗炎、抗氧化、镇痛活性和较弱的抗分枝杆菌活性。DL-Syringaresinol 可通过自噬延缓氧化应激诱导的皮肤老化，通过抑制炎症反应来缓解奥沙利铂诱导的神经性疼痛和脓毒症引起的心功能障碍。
TMS1461	Qingyangshengenin B 青阳参甙元B,青阳参苷元B,Otophylloside B	Beta Amyloid	Neuroscience
	Qingyangshengenin B (Otophylloside B) 是一种分离自 Qingyangshen 的 C-21 甾体苷。它能够在 mRNA 水平上抑制 Aβ 的表达来减少 Aβ 的沉积，对 Aβ 的毒性有保护作用。它具有抗癫痫作用。
T4716	Pyrrole-2-carboxylic acid 吡咯-2-羧酸,2-Pyrrolecarboxylic acid,Minaline	Endogenous Metabolite	Metabolism
	Pyrrole-2-carboxylic acid (Minaline) 是一种天然生物碱类，从海洋细菌Pelomonas puraquaesp. Nov 中分离得到。
T4776	Glycerol Glycerin,甘油	Endogenous Metabolite	Metabolism
	Glycerol 是甘油三酯（即脂肪和油）和磷脂的重要成分。它在食品工业中被广泛用作甜味剂和保湿剂以及药物制剂。
TN4173	Guajadial C	Topoisomerase	DNA Damage/DNA Repair
	Guajadial C acts as a Top1 catalytic inhibitor and can delay Top1 poison-mediated DNA damage. It shows cytotoxicity against five human cancer cell lines.
TN5348	Guajadial F
	Guajadial F acts as a Top1 catalytic inhibitor and can delay Top1 poison-mediated DNA damage. Guajadial F shows cytotoxicity against five human cancer cell lines.
TN2839	2alpha,19alpha-Dihydroxy-3-oxo-urs-12-en-28-oic acid	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	2alpha,19alpha-Dihydroxy-3-oxo-urs-12-en-28-oic acid has anti-HIV activity. It shows an inhibitory effect on the activation of Epstein-Barr virus early antigen (EBV-EA) induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) and causes a significant delay o

天然产物

Scutellarin methyl ester

Cat.No: T2S0842

Synonym: Scutellarin methylester,野黄芩苷甲酯

Target: Others

2-Methylsuccinic acid

Cat.No: T5231

Synonym: Pyrotartaric Acid,Methylbutanedioic acid,甲基丁二酸

Target: Others, Endogenous Metabolite

Cat.No: T3864

Target: BCL, Antibacterial

DL-Syringaresinol

Cat.No: TN1594

Synonym: (±)-Syringaresinol

Target: Antioxidant, Antifungal

Qingyangshengenin B

Cat.No: TMS1461

Synonym: 青阳参甙元B,青阳参苷元B,Otophylloside B

Target: Beta Amyloid

Pyrrole-2-carboxylic acid

Cat.No: T4716

Synonym: 吡咯-2-羧酸,2-Pyrrolecarboxylic acid,Minaline

Target: Endogenous Metabolite

Cat.No: T4776

Synonym: Glycerin,甘油

Target: Endogenous Metabolite

Cat.No: TN4173

Target: Topoisomerase

Cat.No: TN5348

2alpha,19alpha-Dihydroxy-3-oxo-urs-12-en-28-oic acid

Cat.No: TN2839

Target: HIV Protease

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