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37

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11399	Giredestrant GDC-9545	Estrogen Receptor/ERR; Estrogen/progestogen Receptor	Endocrinology/Hormones
	Giredestrant (GDC-9545) 是一种口服有效的、选择性的、非甾体的雌激素受体 (ER) 拮抗剂，具有抗肿瘤作用。它可以在 ER 配体结合域内与雌二醇 (Estradiol) 竞争结合并诱导构象变化。
T125179	Archangelicin
	Archangelicin 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 T125179，CAS号为 2607-56-9。
T25373	EMD57439 EMD-57439,EMD 57439	PDE	Metabolism
	EMD57439是一种选择性的PDE-III 抑制剂，对c-AMP 浓度没有显示出明显的增长且在Ca(50)中产生的变化很小。
T16859	SBI-425	Others	Others
	SBI-425 是一种有效且具有口服生物利用度的 TNAP 抑制剂。 SBI-425 有效抑制脉管系统中的 TNAP，改善心血管参数和存活率，而骨骼没有检测到变化。
T11179	Elubrixin SB-656933	IL Receptor; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Elubrixin (SB-656933) 是一种有效和特异性的 CXCR2 和 IL-8 受体拮抗剂。 Elubrixin 可用于炎症性疾病的研究，例如炎症性肠病和气道炎症。
T8799	(E/Z)-IT-603 IT603	Others; NF-κB	NF-κB; Others
	(E/Z)-IT-603 是一种c-Rel 抑制剂，其IC50=3 μM。它是 E-IT-603 和 Z-IT-603的混合物。它具有抗癌作用。它有望作为调节剂调节移植物抗宿主病和恶性病中的 T 细胞反应。
T35353	Elubiol dichlorophenyl imidazoldioxolan,新康唑	Antibacterial	Microbiology/Virology
	Elubiol (dichlorophenyl imidazoldioxolan) 是咪唑类的新型广谱抗真菌产品，可抑制真菌麦角甾醇的生物合成，改变细胞膜中其他脂质化合物的组成。 Elubiol 用于油性皮肤或头皮屑患者的皮肤和头发护理。
T6778	BDA-366	BCL	Apoptosis
	BDA-366 是一种有效的 Bcl2 拮抗剂，以高亲和力和选择性 (Ki = 3.3 nM) 结合 Bcl2-BH4 结构域。 BDA-366 诱导 Bcl2 的构象变化，从而消除其抗凋亡功能，将其从存活分子转变为细胞死亡诱导剂。 BDA-366 抑制肺癌细胞的生长。
T19658	Enflurane NSC115944,Ethrane,NSC-115944,恩氟烷,Efrane,NSC 115944	Others	Others
	Enflurane (Efrane) 是一种挥发性麻醉剂，是 Chara australis 高电导 Ca2+ 激活的 K+ 通道的有效抑制剂。安氟醚是通过顶空气相色谱-质谱法监测卤化挥发性麻醉剂的内标。它可以快速调整麻醉深度，而脉搏或呼吸频率几乎没有变化。
T31495	Dimethylmyleran
	Dimethylmyleran can promote Haematological change and affect spermatogenesis.
T71989	CPD7 HCl
	CPD7 HCl is a novel non-RBD binding modulator to inhibit SARS-CoV-2 by prohibiting the conformational change of the spike (S) protein.
T69252	CPD26
	CPD26 is a novel non-RBD binding modulator to inhibit SARS-CoV-2 by prohibiting the conformational change of the spike (S) protein.
T68310	CPD7
	CPD7 is a novel non-RBD binding modulator to inhibit SARS-CoV-2 by prohibiting the conformational change of the spike (S) protein.
T24740	RS-104966
	RS-104966 is an inhibitor of collagenase that acts by inducing the conformational change in the side-chains of the S1 pocket of MMP-1.
T36932	CD532 hydrochloride
	CD532 hydrochloride is a potent inhibitor of Aurora A kinase, having an IC50 of 45 nM. It not only blocks the activity of Aurora A kinase but also facilitates the degradation of the protein MYCN. Furthermore, CD532 hydrochloride interacts directly with AURKA, inducing a significant conformational change. Its utility in cancer research has been demonstrated [1][2].
T15565	Imetit dihydrobromide VUF 8325 dihydrobromide,SKF 91105 dihydrobromide	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Imetit dihydrobromide is a high affinity and effective agonist of histamine H3 and H4 receptors (Ki: 0.3 and 2.7 nM). Imetit mimics the histamine effect in triggering a shape change in eosinophils (EC50: 25 nM).
T28099	MRS2179 MRS 2179,MRS-2179
	MRS2179 is a competitive P2Y1 receptor antagonist (Kb = 100 nM) with no appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 µM, or at P2Y12 and P2Y13. It inhibits ADP-induced platelet shape change and aggregation (pA2 = 6.55) in vitro a
T41204	TAT-Gap19(I130A) TAT-Gap19(I130A)
	TAT-Gap19(I130A) is a control peptide for TAT-Gap19, a Cx43 hemichannel blocker. TAT-Gap19(I130A) consists of TAT-GAP19 with a I130A amino acid residue change at a key residue for GAP19 activity. In C6 glioma cells expression Cx43, TAT-GAP19(1130A) does not inhibit [Ca2+]i-triggered ATP release at 200 μM. TAT-Gap19(I130A) is cell permeable.
T38952	Triperiden
	Triperiden is a chemical compound that serves as an inhibitor of influenza virus multiplication. Specifically, it exerts its antiviral activity by targeting the haemagglutinin of fowl plague virus (FPV) and inhibiting the conformational change in the haemagglutinin at acid pH. Additionally, Triperiden is classified as an anticholinergic anti-parkinsonism drug.
T68413	CBS1194
	CBS1194 is a novel antiviral agent against influenza A virus (IAV), and is more specifically, a group 2 IAV fusion inhibitor. CBS1194 prevents membrane fusion of the virus through the inhibition of the conformational change of hemagglutinin (HA). CBS1194 causes steric hinderance that prevents the rearrangement of the HA that would normally be induced by low-pH, by fitting into the pocket by the fusion peptide.
T30078	ANNINE-6plus
	ANNINE-6plus is a water soluble voltage sensitive dye (also called potentiometric dyes). This compound was developed at the Max Planck Institute for Biochemistry in Germany. It is used to optically measure the changes in transmembrane voltage of excitable
T78434	Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide (human) TFA
	Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide (human) TFA 为基于荧光共振能量转移的多肽底物，通过裂解引起的荧光强度变化来确定其活性。
T82612	Dansyl ethylenediamine
	Dansyl ethylenediamine是一种用于合成能特异地转导蛋白质结合事件为荧光信号变化的蛋白质印迹聚合物的荧光探针。
T41121	Elubrixin tosylate SB-656933 tosylate,Elubrixin tosylate
	Elubrixin tosylate (SB-656933 tosylate) is a high-potency, selective, competitive, and reversible CXCR2 antagonist, as well as an antagonist of the IL-8 receptor. It effectively inhibits upregulation of neutrophil CD11b (with an IC50 of 260.7 nM) and shape change (with an IC50 of 310.5 nM). This compound holds promise for the study of inflammatory diseases, including inflammatory bowel disease and airway inflammation.
T36164	8-iso Prostaglandin F3α 8-iso Prostaglandin F3α,8-epi PGF3α
	8-iso PGF3α is an isoprostane produced from the free-radical peroxidation of EPA. Little is known about the biological activity of 8-iso PGF3α. There is one report that it is inactive in a TP receptor mediated assay of human platelet shape change, where 8-iso PGF2α has an ED50 value of 1 uM. [1]
T82524	Dual photoCORM 1
	Dual photoCORM 1（化合物 5）是一种无金属的光化学活性双CORM，它不仅展现出良好的细胞摄取性能，还能实时监测CO的释放。
T72988	photoCORM-2
	photoCORM-2 是一种单一的一氧化碳释放分子 (CORM)，photoCORM-2 表现出良好的细胞吸收和通过颜色变化方法实时监测 CO 解锁的能力。photoCORM-2 具有抗肿瘤活性。
T81838	Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide (human)
	Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide (human) 为一种基于FRET (荧光共振能量转移) 原理的多肽底物，通过其裂解引起的荧光强度变化来评估其活性。
T35586	I-SAP
	I-SAP is a high affinity TP receptor antagonist. At physiologic pH, I-SAP produces platelet shape change, but not aggregation, with an EC50 value of 9.7 nM. I-SAP binds to human platelets with the maximum binding obtained between pH 6.5 and pH 7.4. In washed human platelets, the Kd for I-SAP is 468 pM at pH 7.4 and 490 pM at pH 6.5.
T10462L	Bavisant dihydrochloride hydrate JNJ31001074AAC	Others	Others
	Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change
T80705	α-Naphtholbenzein p-Naphtolbenzein
	α-Naphtholbenzein (p-Naphtolbenzein) 是一种可作为pH指示剂使用的染料，具有pH0至8.2范围内呈现黄色、pH10时转变为青绿色的视觉过度特性，常应用于酸碱滴定。
T72987	photoCORM-1
	photoCORM-1 是一种组合式一氧化碳释放分子 (CORM)。photoCORM-1 表现出良好的细胞吸收和通过颜色变化方法实时监测 CO 释放的能力。photoCORM-1 具有抗肿瘤活性。
T36988	N-(3-hydroxy-7-cis tetradecenoyl)-L-Homoserine lactone
	N-(3-hydroxy-7-cis tetradecenoyl)-L-Homoserine lactone is a long-chain N-acyl-homoserine lactone (AHL) produced by some Gram-negative bacteria and is involved in quorum sensing. Quorum sensing enables bacteria to change gene expression based on cues from nearby bacteria and from eukaryotic hosts about nutrients, environmental conditions, or threats. Due to the benefit of quorum sensing for bacterial survival, quorum sensing molecules are potential targets for controlling bacterial infections. In...
T68981	PD-321852
	PD-321852 is a small-molecule Chk1 inhibitor, which potentiates gemcitabine-induced clonogenic death in a panel of pancreatic cancer cell lines and evaluated the relationship between endpoints associated with Chk1 inhibition and chemosensitization. Gemcitabine chemosensitization by minimally toxic concentrations of PD-321852 ranged from minimal (<3-fold change in survival) in Panc1 cells to >30-fold in MiaPaCa2 cells. PD-321852 inhibited Chk1 in all cell lines as evidenced by stabilization of Cd...
T68499	F15845 HBr
	F 15845 is a blocker of the persistent sodium current prevents consequences of hypoxia in rat femoral artery. F15845 has been shown to selectively inhibit the persistent sodium current of Nav1.5[1] exerting cardioprotective effects following ischemia. In vitro testing showed minimal effects of F15845 on other important ion channels of the heart, including major Ca2+ and K+ channels.[1] This characteristic is thought to account for the limited effect of F15845 to change other heart parameters suc...
T68219	Peraclopone
	Peraclopone is a hypolidemic drug. It is an inhibitor of 7-Dehydrocholesterol reductase. Peraclopone potently inhibits the final step in cholesterol biosynthesis. Feeding this agent to rats leads to a rapid replacement of membrane cholesterol with its immediate precursor 7-dehydrocholesterol, and a dramatic reduction in plasma sterol concentration. Peraclopone caused a dose-dependent decrease in cholesterol and a concomitant accumulation of provitamin D3 (7-dehydrocholesterol) in the skin, which...
T39656	BDY FL-X, SE
	BODIPY FL-X,SE is a fluorescent green dye for the labeling of amine , shows a high fluorescence quantum yield and is relatively insensitive to pH change. BODIPY FL-X,SE can be used as an alternative for FAM, Cy2 or FITC. λ abs : 504 nm; λ em :510 nm.

化合物

Cat.No: T11399

Synonym: GDC-9545

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

Cat.No: T125179

Cat.No: T25373

Synonym: EMD-57439,EMD 57439

Target: PDE

Cat.No: T16859

Target: Others

Cat.No: T11179

Synonym: SB-656933

Target: IL Receptor, CXCR

Cat.No: T8799

Synonym: IT603

Target: Others, NF-κB

Cat.No: T35353

Synonym: dichlorophenyl imidazoldioxolan,新康唑

Target: Antibacterial

Cat.No: T6778

Target: BCL

Cat.No: T19658

Synonym: NSC115944,Ethrane,NSC-115944,恩氟烷,Efrane,NSC 115944

Target: Others

Dimethylmyleran

Cat.No: T31495

Cat.No: T71989

Cat.No: T69252

Cat.No: T68310

Cat.No: T24740

CD532 hydrochloride

Cat.No: T36932

Imetit dihydrobromide

Cat.No: T15565

Synonym: VUF 8325 dihydrobromide,SKF 91105 dihydrobromide

Target: Histamine Receptor

Cat.No: T28099

Synonym: MRS 2179,MRS-2179

TAT-Gap19(I130A)

Cat.No: T41204

Synonym: TAT-Gap19(I130A)

Cat.No: T38952

Cat.No: T68413

Cat.No: T30078

Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide (human) TFA

Cat.No: T78434

Dansyl ethylenediamine

Cat.No: T82612

Elubrixin tosylate

Cat.No: T41121

Synonym: SB-656933 tosylate,Elubrixin tosylate

8-iso Prostaglandin F3α

Cat.No: T36164

Synonym: 8-iso Prostaglandin F3α,8-epi PGF3α

Dual photoCORM 1

Cat.No: T82524

Cat.No: T72988

Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide (human)

Cat.No: T81838

Cat.No: T35586

Bavisant dihydrochloride hydrate

Cat.No: T10462L

Synonym: JNJ31001074AAC

Target: Others

α-Naphtholbenzein

Cat.No: T80705

Synonym: p-Naphtolbenzein

Cat.No: T72987

N-(3-hydroxy-7-cis tetradecenoyl)-L-Homoserine lactone

Cat.No: T36988

Cat.No: T68981

Cat.No: T68499

Cat.No: T68219

Cat.No: T39656

Cat. No.	Product Name	Target	Signaling Pathways
T5S1261	Methylophiopogonanone B	Ras	GPCR/G Protein; MAPK
	Methylophiopogonanone B 是一种高异二氢黄酮，提取自麦冬的根，抗氧化能力强，它通过 Rho 信号传导途径及增加 GTP-Rho 发挥效果。它能够重组肌动蛋白细胞骨架，使细胞形态（如树突收缩、应力纤维形成）发生变化。
T3237	Lecithin Phospholutein,卵磷脂,L-α-磷脂酰胆碱,L-α-Phosphatidylcholine,Phosphatidylcholines	Others; Endogenous Metabolite	Metabolism; Others
	Lecithin (L-α-Phosphatidylcholine) 被认为是安全的常规磷脂源。磷脂能够改变动物细胞膜的脂肪酸组成和微观结构。
T4713	Phosphorylcholine chloride calcium salt tetrahydrate Phosphocholine chloride calcium salt tet,胆碱磷酸氯化钙四水,CalciuM Phosphorylcholine Tetrahydrate	Others; Endogenous Metabolite	Metabolism; Others
	Phosphorylcholine chloride calcium salt tetrahydrate (Phosphocholine chloride calcium salt tet) 是内源性代谢产物的一种。
T5S0527	Rhodojaponin III 闹羊花素 Ⅲ,闹羊花毒素III	Others	Others
	Rhodojaponin III 是二萜类化合物，提取于Rhododendron molle 叶子，具有抗炎作用。
TN1208	2-Amino-3-carboxy-1,4-naphthoquinone	NADPH-oxidase	Immunology/Inflammation
	2-Amino-3-carboxy-1,4-naphthoquinone 是电子转移介质，可改变同型发酵乳酸菌的葡萄糖代谢，可作为双歧杆菌生长刺激剂，它通过NAD(P)H 介导的氧化作用影响双歧杆菌的终产物形态。

天然产物

Methylophiopogonanone B

Cat.No: T5S1261

Target: Ras

Cat.No: T3237

Synonym: Phospholutein,卵磷脂,L-α-磷脂酰胆碱,L-α-Phosphatidylcholine,Phosphatidylcholines

Target: Others, Endogenous Metabolite

Phosphorylcholine chloride calcium salt tetrahydrate

Cat.No: T4713

Synonym: Phosphocholine chloride calcium salt tet,胆碱磷酸氯化钙四水,CalciuM Phosphorylcholine Tetrahydrate

Target: Others, Endogenous Metabolite

Rhodojaponin III

Cat.No: T5S0527

Synonym: 闹羊花素 Ⅲ,闹羊花毒素III

Target: Others

2-Amino-3-carboxy-1,4-naphthoquinone

Cat.No: TN1208

Target: NADPH-oxidase

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