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24

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7469	Alendronic Acid alendronate,阿仑膦酸	Others	Others
	Alendronic Acid (alendronate) 是法呢基二磷酸合酶(FDPS)抑制剂，是一种双膦酸盐。它能够抑制破骨细胞介导的骨吸收，对绝经后骨质疏松症，恶性高钙血症和 Paget 病具有疗效。
T1850	Balicatib AAE581,巴利卡替	Cysteine Protease	Proteases/Proteasome
	Balicatib (AAE581) 是组织蛋白酶K 抑制剂，其对组织蛋白酶K 的抑制作用是组织蛋白酶B、L 和S 的抑制性的10到100倍。
T20319	Pentabromophenol 五溴苯酚,NSC 5717,NSC5717,NSC-5717	TGF-beta/Smad	Stem Cells
	Pentabromophenol (NSC-5717) 通过加速 TGF-β 受体的转换率来抑制 TGF-β 反应。
T24612	Pentachloropseudilin PClP
	Pentachloropseudilin is a selective inhibitor of Myosin-1. In target cells, It acts by suppressing transforming growth factor-β activity by accelerating cell-surface type II TGF-β receptor turnover.
T0308	Etidronic acid HEDPA,Etidronate,HEDP,羟乙磷酸	Apoptosis; Phosphatase; Others; HBV	Apoptosis; Metabolism; Microbiology/Virology; Others
	Etidronic acid (HEDP) 是一种影响钙代谢的二膦酸盐，抑制异位钙化并减缓骨吸收和骨转换，可应用于洗涤，水处理，化妆品和制药业。
T14984	CLP257	Potassium Channel	Membrane transporter/Ion channel
	CLP257 是有效的 K+-Cl- 协同转运蛋白 KCC2 选择性激活剂 (EC50: 616 nM)。它可减轻神经性疼痛大鼠的超敏反应，并在翻译后调节质膜 KCC2 蛋白周转。它在 KCC2 活性降低的神经元中恢复受损的 Cl- 转运。
T19649	PF-06273340 PF 6273340,PF 06273340,PF6273340,PF-6273340	Trk receptor	Tyrosine Kinase/Adaptors
	PF-06273340 是一种口服具有活力的、具有选择性的外周限制性Trk 泛抑制剂。
T77581	KM02894	GluR	Neuroscience
	KM02894 是一种谷氨酸释放抑制剂。癌细胞释放高水平的谷氨酸，能够破坏正常的骨转换，这可能导致癌症引起的骨痛。KM02894 可用于研究肿瘤相关疾病。
T1631	Sulbactam CP45899,舒巴坦,舒巴坦酸	Antibacterial; Antibiotic	Microbiology/Virology
	Sulbactam (CP45899) 是一种竞争性、不可逆的 β-内酰胺酶抑制剂，抑制耐多药不动杆菌-鲍曼不动杆菌复合物。它具有抗菌活性。
T36971	5-Ethynyluridine	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	5-Ethynyluridine 可用于标记新合成的 RNA。这种方法称为使用点击化学 (RICK) 捕获新转录的 RNA 相互作用组，系统地捕获与多种 RNA 结合的蛋白质，包括新生 RNA 和传统上被忽视的非多腺苷酸化 RNA。
T36949	Niaprazine	5-HT Receptor; Adrenergic Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Niaprazine 是有效的组胺 H1 受体拮抗剂，具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。
T70983	Zoledronate disodium
	Zoledronate disodium is an inhibitor of osteoclastogenesis and macrophage recruitment, decreasing bone turnover and stabilizing the bone matrix, exhibiting diverse anti-tumor effects in osteosarcoma.
T31940	Glucosylgalactosylhydroxylysine Hydroxylysine-glucose-galactose
	Glucosylgalactosylhydroxylysine is a bone formation and bone resorption marker that is related to bone turnover processes during growth and development as well as metabolic bone diseases.
T60368	Benzoctamine
	Benzoctamine 是一种口服有效作用精神剂，具有镇静作用。Benzoctamine 增加儿茶酚胺的周转率。Benzoctamine 增强大鼠心脏中 [3H] 去甲肾上腺素的摄取。Benzoctamine 也可加速脑内注射 [3H] 去甲肾上腺素的消失。
T15455	RGH-5526 GYKI-11679	Others	Others
	RGH-5526是一种新型的抗高血压药。它引起下丘脑去甲肾上腺素（NA）周转（利用）增加，下丘脑去甲肾上腺素能神经元活性的增加可能导致外周交感神经活性的降低，从而显著降低血压。
T36191	CAY10681
	Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling. It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53. CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65. It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 μM). CAY10681 exhibits excellent oral bioavailability and...
T76113	Creatine kinase (OcCK)
	Creatine kinase (OcCK) 催化肌酸和 ATP 的可逆反应，形成磷酸肌酸和 ADP。Creatine kinase (OcCK) 是在快速能量周转期间维持恒定 ATP/ADP 比率的关键酶。
T39916	GNE-274
	GNE-274, a non-degrader compound structurally similar to GDC-0927 (an ER degrader), serves as a partial ER agonist in breast cancer cell lines without triggering ER turnover. Notably, GNE-274 enhances chromatin accessibility at ER-DNA binding sites, unlike GDC-0927. Acting as a potent inhibitor of the ER-ligand binding domain (LBD), GNE-274 exhibits potential for cancer research purposes.
T68976	Piragliatin
	Piragliatin, also known as RO4389620, is a glucokinase activator. Piragliatin greatly enhances glucose-induced pancreatic islet respiration and insulin release. Piragliatin lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus. Piragliatin has an acute glucose-lowering action in patients with mild type 2 diabetes, mainly mediated through a generalized enhancement of β-cell function and through fasting restricted changes in ...
T11798	L-692429 MK-0751	GHSR; GPCR19	GPCR/G Protein
	L-692429 (MK-0751) 是一种有效的非肽基生长激素促分泌素 (GHS) 激动剂，是一种苯并内酰胺的衍生物，可逆转糖皮质激素对 GH 分泌的抑制。L-692429 对 G 蛋白偶联受体 (G protein-coupled receptor)具有很高的亲和力，可用于研究肢端肥大症和肥胖。
T35604	Osteocalcin (1-49) (human) (trifluoroacetate salt)
	Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in w...
T35553	Ganglioside GQ1b Mixture (sodium salt)
	Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit. It stimulates phosphorylation of several ecto-type protein kinase substrates on the surface of GOTO human neuroblastoma cells when used at a concentration of 5 nM. Ganglioside GQ1b promotes differentiation of murine embryonic stem cells (mESCs) to neuronal precursor and glial cells via activation of the ERK1/2 pathway. It also induces differentiation of murine keratinocytes throu...
TP2301	type II collagen fragment	Others	Others
	Type II collagen is composed of a triple helix of three identical α chains. These molecules associate to form a fibril that is stabilized by intermolecular crosslinks1. Damage to the fibrillar meshwork, made up of primarily type II collagen (z 90–95%), ma
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...

化合物

Alendronic Acid

Cat.No: T7469

Synonym: alendronate,阿仑膦酸

Target: Others

Cat.No: T1850

Synonym: AAE581,巴利卡替

Target: Cysteine Protease

Pentabromophenol

Cat.No: T20319

Synonym: 五溴苯酚,NSC 5717,NSC5717,NSC-5717

Target: TGF-beta/Smad

Pentachloropseudilin

Cat.No: T24612

Synonym: PClP

Cat.No: T0308

Synonym: HEDPA,Etidronate,HEDP,羟乙磷酸

Target: Apoptosis, Phosphatase, Others, HBV

Cat.No: T14984

Target: Potassium Channel

Cat.No: T19649

Synonym: PF 6273340,PF 06273340,PF6273340,PF-6273340

Target: Trk receptor

Cat.No: T77581

Target: GluR

Cat.No: T1631

Synonym: CP45899,舒巴坦,舒巴坦酸

Target: Antibacterial, Antibiotic

5-Ethynyluridine

Cat.No: T36971

Target: Nucleoside Antimetabolite/Analog

Cat.No: T36949

Target: 5-HT Receptor, Adrenergic Receptor, Histamine Receptor

Zoledronate disodium

Cat.No: T70983

Glucosylgalactosylhydroxylysine

Cat.No: T31940

Synonym: Hydroxylysine-glucose-galactose

Cat.No: T60368

Cat.No: T15455

Synonym: GYKI-11679

Target: Others

Cat.No: T36191

Creatine kinase (OcCK)

Cat.No: T76113

Cat.No: T39916

Cat.No: T68976

Cat.No: T11798

Synonym: MK-0751

Target: GHSR, GPCR19

Osteocalcin (1-49) (human) (trifluoroacetate salt)

Cat.No: T35604

Ganglioside GQ1b Mixture (sodium salt)

Cat.No: T35553

type II collagen fragment

Cat.No: TP2301

Target: Others

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Cat. No.	Product Name	Target	Signaling Pathways
T8112	β-Gentiobiose	Others	Others
	β-Gentiobiose 是一种能够促进果实成熟天的然寡糖。
TN2019	Orobol 3'-Hydroxygenistein,3’,4’,5,7-tetrahydroxy-isoflavon,3',4',5,7-四羟基异黄酮	BCL; Caspase; PI3K	Apoptosis; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Orobol (3’,4’,5,7-tetrahydroxy-isoflavon) 是酪氨酸特异性蛋白激酶和磷脂酰肌醇转换的抑制剂。Orobol 抑制 PI3K，对 PI3K α/β/γ/K/δ 的 IC50 为 3.46-5.27 μM。 Orobol 具有抗皮肤老化和抗肥胖的作用。
T2820	Glycitin 黄豆黄苷,Glycitein-7-β-O-glucoside,Glycitein 7-O-β-glucoside	Others; Influenza Virus; Antibacterial	Microbiology/Virology; Others
	Glycitin (Glycitein 7-O-β-glucoside) 是一种从豆类中分离出来的天然异黄酮，有抗菌，抗病毒和雌激素作用，还有促进骨髓基质细胞和成骨细胞的增殖和抑制骨转换的生物学功能。
T4746	Purine 7H-Imidazo(4,5-d)pyrimidine,嘌呤	Others; Endogenous Metabolite	Metabolism; Others
	Purine (7H-Imidazo(4,5-d)pyrimidine) 是内源性代谢产物的一种。
T6S2140	β-Anhydroicaritin Anhydroicaritin,Beta-Anhydroicaritin,脱水淫羊藿素	MMP; Others; TNF; Interleukin	Apoptosis; Immunology/Inflammation; Others; Proteases/Proteasome
	β-Anhydroicaritin 是从乳香提取的一种天然产物，具有重要的生物学和药理学作用，如抗骨质疏松症，雌激素调节和抗肿瘤特性。它改善牙周组织的降解，抑制糖尿病大鼠 TNF-α 和 MMP-3 的合成和分泌。它抑制细胞内 Ca2+的升高，并显著降低 iNOS 蛋白的表达。

天然产物

Cat.No: T8112

Target: Others

Cat.No: TN2019

Synonym: 3'-Hydroxygenistein,3’,4’,5,7-tetrahydroxy-isoflavon,3',4',5,7-四羟基异黄酮

Target: BCL, Caspase, PI3K

Cat.No: T2820

Synonym: 黄豆黄苷,Glycitein-7-β-O-glucoside,Glycitein 7-O-β-glucoside

Target: Others, Influenza Virus, Antibacterial

Cat.No: T4746

Synonym: 7H-Imidazo(4,5-d)pyrimidine,嘌呤

Target: Others, Endogenous Metabolite

β-Anhydroicaritin

Cat.No: T6S2140

Synonym: Anhydroicaritin,Beta-Anhydroicaritin,脱水淫羊藿素

Target: MMP, Others, TNF, Interleukin

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