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22

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T14364	AZ-Dyrk1B-33 3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine	DYRK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) 是高选择性的Dyrk1B 激酶抑制剂，其IC50=7 nM。
TP1236	Etelcalcetide hydrochloride AMG 416 hydrochloride,维考西肽盐酸盐,KAI-4169 hydrochloride	CaSR	GPCR/G Protein
	Etelcalcetide hydrochloride (AMG 416 hydrochloride) 是具有有钙敏感受体 (CaSR) 活化剂作用的合成肽，能够减少接受血液透析的继发性甲状旁腺功能亢进患者的甲状旁腺激素 (PTH) 浓度。
T0230	Prasugrel LY640315,CS-747,普拉格雷,PCR 4099	P2Y Receptor	GPCR/G Protein; Neuroscience
	Prasugrel (CS-747) 是一种噻吩吡啶和前药，是一种可口服的 P2Y12受体拮抗剂，抑制 ADP 诱导的血小板聚集，用于预防急性冠状动脉综合征患者的血栓形成、不稳定型心绞痛和心肌梗塞，以及接受经皮冠状动脉介入治疗的患者。
T3614	Inosine pranobex Groprinosin,Isoprinosine,异丙肌苷,Immunovir,Delimmun	IL Receptor; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Inosine pranobex (Delimmun) 是一种免疫增强剂，它是一种广谱抗病毒剂，用于 HIV 感染。
T21537L	TMC647055 Choline Hydroxide Salt TMC647055 Choline Hydroxide Salt (1204416-97-6 free base)	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	TMC647055 Choline Hydroxide Salt 是一种新型有效的 HCV NS5B 聚合酶非核苷抑制剂，可用于治疗 HCV 感染。它具有纳摩尔级细胞效力（EC(50) 为 82 nM），相关细胞毒性较小（CC(50)>20 μM），在大鼠和狗中具有良好的药代动力学特征。 TMC647055 显示出有体外生化、动力学和病毒学特征的前景。
T68312	Etanterol
	Etanterol is a phenethanolamine derivative and a β2 adrenoceptor agonist that was undergoing phase II trials in Italy as a bronchodilator with Valeas.
T69960	CJ-15161 hydrochloride
	CJ-15161 hydrochloride is the salt form of CJ-15161 (free base), an opioid κ-receptor agonist, is undergoing development with Pfizer as an analgesic agent.
T69961	CJ-15161 (free base)
	CJ-15161 (free base), an opioid κ-receptor agonist, is undergoing development with Pfizer as an analgesic agent.
T71154	SX-576
	SX-576 is undergoing further investigation as a potential therapy for pulmonary inflammation. It is also a potent non-competitive boronic acid-containing CXCR1/2 antagonists.
T6287L	Tariquidar dimesylate D 06008,XR9576,D06008,XR 9576,Tariquidar dimesilate,XR-9576
	Tariquidar is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs.
T69557	ABI-231 HCl
	ABI-231 is a potent, orally bioavailable tubulin inhibitor that interacts with the colchicine binding site and is currently undergoing clinical trials for prostate cancer. ABI-231, has an average IC50 = 5.2 nM against panels of melanoma and prostate cancer cell lines, is orally bioavailable, and strongly suppress melanoma tumors in vivo. ABI-231 holds great promise as a new generation of orally available tubulin inhibitor.
T12610	(R)-3-Hydroxy Midostaurin (R)-CGP52421	Others	Others
	(R)-3-Hydroxy Midostaurin is a potent inhibitor of kinases,is a major metabolite of midostaurin undergoing by the hepatic CYP3A4 enzyme,has the potential for acute myeloid leukemia (AML).
TP1235	Etelcalcetide AMG 416,KAI-4169
	Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is a calcimimetic drug for the treatment of secondary hyperparathyroidism in patients undergoing hemodialysis.
T17026L	Tecovirimat hydrate ST246,ST 246,ST-246,SIGA 246,SIGA246,SIGA-246
	Tecovirimat,(ST-246, SIgA-246) is an inhibitor of p37 envelope proteins used to treat smallpox infection. Tecovirimat is an antiviral drug that is active against orthopoxviruses such as smallpox and is currently undergoing clinical trials. Its role is to
T37437	C17 Ceramide (d18:1/17:0)
	C17 Ceramide is a synthetic ceramide that contains a non-natural C17:0 fatty acid acylated to sphingosine. It has been used as a marker of arylsulfatase A and sphingolipid activator B activity in patients undergoing enzyme replacement therapy for the genetic disease metachromatic leukodystrophy.
T68639	Ciprostene (free base)
	Ciprostene (free base) is a synthetic, chemically stable analog of prostacyclin (PGI2). In animal models, administration of ciprostene resulted in dose-dependent hypotension, tachycardia, and inhibition of ex vivo ADP-induced platelet aggregation. Ciprostene was evaluated in clinical trials in patients with peripheral vascular disease. It was found to reduce restenosis in patients with coronary artery disease undergoing therapeutic percutaneous transluminal coronary angioplasty.
T82006	JM3A
	JM3A为高特异性生物活性肽，针对早期肺癌细胞转化过程中新表达的细胞表面波形蛋白(CSV)。通过与荧光团耦合，JM3A能够检测并标记CSV。
T82654	Cy3-PEG3-TCO4
	Cy3-PEG3-TCO4为Cyanine 3 (Cy3) 染料的PEG衍生物，含有3个PEG链段。该化合物通过TCO基团与含Tetrazine基团的靶分子实现逆电子需求 Diels-Alder 反应 (iEDDA)。
T71549	RKS-262
	RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several...
T83872	Oleoyl-L-carnitine chloride L-Carnitine oleoyl ester,L-Octadecanoylcarnitine,C18:1 Carnitine,CAR 18:1
	Oleoyl-L-carnitine是一种长链酰基肉碱，也是一种糖苷转运体2（GlyT2；IC50 = 340 nM）的抑制剂，对GlyT2比对GlyT1（IC50 = >10,000 nM）具有选择性。慢性肾脏病或接受初始血液透析的终末期肾脏病患者的血浆中Oleoyl-L-carnitine水平增高，这与心血管死亡率相关。
T72213	Efonidipine hydrochloride NZ-105 hydrochloride
	Efonidipine(NZ-105)盐酸盐是T 型和L 型钙离子通道双重阻断剂。
T83798	8-bromo NAD+ sodium 8-bromo Nicotinamide adenine dinucleotide,N(8-bromo-A)D+
	8-bromo NAD+ 作为循环ADP-核糖（cADPR）抑制剂8-bromo cADPR的前药形式，通过CD38转化为8-bromo-cADPR。在1 mM浓度下，8-bromo NAD+ 阻止由N-formyl-Met-Leu-Phe (fMLP) 在分离的小鼠骨髓衍生的中性粒细胞内引起的细胞内钙水平增加和趋化作用。同时，在100 µM浓度下使用，减少了小鼠原代小胶质细胞中LPS诱导的亚硝酸盐产生以及TNF-α和IL-2的分泌。

化合物

Cat.No: T14364

Synonym: 3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine

Target: DYRK

Etelcalcetide hydrochloride

Cat.No: TP1236

Synonym: AMG 416 hydrochloride,维考西肽盐酸盐,KAI-4169 hydrochloride

Target: CaSR

Cat.No: T0230

Synonym: LY640315,CS-747,普拉格雷,PCR 4099

Target: P2Y Receptor

Inosine pranobex

Cat.No: T3614

Synonym: Groprinosin,Isoprinosine,异丙肌苷,Immunovir,Delimmun

Target: IL Receptor, HIV Protease

TMC647055 Choline Hydroxide Salt

Cat.No: T21537L

Synonym: TMC647055 Choline Hydroxide Salt (1204416-97-6 free base)

Target: HCV Protease

Cat.No: T68312

CJ-15161 hydrochloride

Cat.No: T69960

CJ-15161 (free base)

Cat.No: T69961

Cat.No: T71154

Tariquidar dimesylate

Cat.No: T6287L

Synonym: D 06008,XR9576,D06008,XR 9576,Tariquidar dimesilate,XR-9576

Cat.No: T69557

(R)-3-Hydroxy Midostaurin

Cat.No: T12610

Synonym: (R)-CGP52421

Target: Others

Cat.No: TP1235

Synonym: AMG 416,KAI-4169

Tecovirimat hydrate

Cat.No: T17026L

Synonym: ST246,ST 246,ST-246,SIGA 246,SIGA246,SIGA-246

C17 Ceramide (d18:1/17:0)

Cat.No: T37437

Ciprostene (free base)

Cat.No: T68639

Cat.No: T82006

Cat.No: T82654

Cat.No: T71549

Oleoyl-L-carnitine chloride

Cat.No: T83872

Synonym: L-Carnitine oleoyl ester,L-Octadecanoylcarnitine,C18:1 Carnitine,CAR 18:1

Efonidipine hydrochloride

Cat.No: T72213

Synonym: NZ-105 hydrochloride

8-bromo NAD+ sodium

Cat.No: T83798

Synonym: 8-bromo Nicotinamide adenine dinucleotide,N(8-bromo-A)D+

Cat. No.	Product Name	Target	Signaling Pathways
T39312	2-Hexylthiophene	Others	Others
	2-Hexylthiophene 是一种碱性极弱的杂芳香族化合物。2-己基噻吩可用于改变和提高钌敏化剂的摩尔吸收系数。
T82799	C-2′-Decoumaroylaloeresin G
	C-2′-Decoumaroylaloeresin G (化合物8)为一种色酮糖苷，源自芦荟属植物。

天然产物

2-Hexylthiophene

Cat.No: T39312

Target: Others

C-2′-Decoumaroylaloeresin G

Cat.No: T82799

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