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25

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16483	PF-05105679	TRP/TRPV Channel	Membrane transporter/Ion channel
	PF-05105679 是一种特异性 TRPM8 拮抗剂 (IC50 = 103 nM)。 PF-05105679 可用于冷相关疼痛的研究。
T9776	TRPM4 inhibitor 8	TRP/TRPV Channel	Membrane transporter/Ion channel
	TRPM4 inhibitor 8 是瞬态受体电位 melastatin 4 (TRPM4) 的抑制剂，它有助于活力、迁移、细胞周期转变和粘附。
T9335	1,1'-Methylenedi-2-naphthol 1，1-亚甲基-2-萘酚,Squoxin	Others	Others
	1,1'-Methylenedi-2-naphthol 靶向 CYP2C19 - 细胞色素 P450 家族 2 亚家族 C 成员 19（人）。
T62204	NR2F6 modulator-1	Others	Others
	NR2F6 modulator-1 是一种核受体亚族 2，F 组第 6 号成员 (NR2F6) 的有效调节剂。NR2F6 modulator-1 能够用于研究免疫调节和肿瘤干细胞活性的调节。
T28020	Mesendogen	TRP/TRPV Channel	Membrane transporter/Ion channel
	Mesendogen 是瞬时受体电位阳离子通道、亚家族 M、成员 6 (TRPM6) 和 7 (TRPM7) 的抑制剂，通过抑制 TRPM6/TRPM7 镁通道活性起作用。
T16745	Rhosin hydrochloride	Apoptosis; Rho; Ras	Apoptosis; Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	Rhosin hydrochloride 是一种特异性 RhoA 亚家族Rho GTPases 抑制剂，抑制 RhoA-GEF 相互作用。它通过增强 D1 中棘神经元的可塑性和降低过度兴奋性来促进应激恢复，可诱导细胞凋亡。
T16763	RN-1747	TRP/TRPV Channel	Membrane transporter/Ion channel
	RN-1747是瞬时受体电位阳离子通道 V 型亚家族成员4（TRPV4 ）的选择性激动剂，对 hTRPV4、mTRPV4 和 rTRPV4 的 EC50分别为0.77 μM、4.0 μM 和4.1 μM。RN-1747也是 TRPM8的拮抗剂，IC50值为4.0 μM。
T10616	BRM/BRG1 ATP Inhibitor-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	BRM/BRG1 ATP Inhibitor-1 是变构双 Brahma 同源物 (BRM)/SWI/SNF 相关的基质相关肌动蛋白依赖性调节剂，染色质亚家族 A 成员 2 和 BRG1/SMARCA4 ATP 酶活性抑制剂，IC50值低于 0.005 μM。
T2024	A-803467 A 803467,A803467	Sodium Channel	Membrane transporter/Ion channel
	A-803467 是有效的、选择性的河豚毒素不敏感型Nav1.8 钠通道阻断剂。它在炎症性疼痛和神经性疼痛模型中有缓解疼痛作用。它通过与 ATP-binding cassette subfamily G member 2 (ABCG2) 转运蛋白的相互作用，增强了传统抗癌物的化疗敏感性。
TP2158	TRV-120027 TFA TRV-120027 TFA (1234510-46-3 free base)	RAAS; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	TRV-120027 TFA 是一种血管紧张素 II 介导的血管收缩抑制剂，可增加心肌细胞的收缩力。它是一种偏向 β-arrestin-1 的 AT1R 激动剂，可与 ß-arrestins 结合，同时阻断 G 蛋白信号传导。它通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌，并促进在质膜上形成由 AT1R-β-arrestin-1-TRPC3-PLCγ 组成的大分子复合物。
T23429	KDM2/7-IN-1 TC-E 5002	Others	Others
	Selective histone demethylase KDM2/7 subfamily inhibitor
T70716	ArgTX-48 TFA
	ArgTX-48 is a highly potent and subfamily selective antagonist of the NMDARs and AMPARs.
T63411	CCG258747
	CCG258747 是一种新型的、选择性的 GRK2 亚家族抑制剂。
T68693	AZ12099548
	AZ12099548 is a transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist.
T71359	ArgTX-93 TFA
	ArgTX-93 is a highly potent and subfamily selective antagonist of the NMDARs and AMPARs.
T82579	Dermaseptin-B9
	Dermaseptin-B9为Phyllomedusinae亚科青蛙分离得到的一种抗菌肽。
T16746	Rhosin	Rho	Cell Cycle/Checkpoint
	Rhosin is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM). Rhosin does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin causes cell apoptosis.
T37086	PDDHV
	PDDHV is a resiniferatoxin-type phorboid vanilloid with capsaicin-like selectivity for the cloned rat transient receptor potential cation channel subfamily V member 1 (TRPV1), formerly known as vanilloid receptor 1. It induces Ca2+-uptake by rat dorsal root ganglion neurons with an EC50 value of 70 nM.
TP2188	type I hair keratin fragment [Homo sapiens]/[Ovis aries]/[Rattus norvegicus]	Others	Others
	The human type I hair keratin subfamily comprises nine individual members, which can be subdivided into three groups. Group A (hHa1, hHa3-I, hHa3-II, hHa4) and B (hHa7, hHa8) each contains structurally related hair keratins, whereas group C members hHa2,
TP2287	Rac GTPase fragment	Others	Others
	Rac GTPase fragment is a peptide with the sequence H2N-Val-Phe-Asp-Glu-Ala-Ile-Arg-Ala-Val-OH, MW= 1019.15. Rac is a subfamily of the Rho family of GTPases, small signaling G proteins (more specifically a GTPase).
T63340	CCG-273220
	CCG-273220 是 G 蛋白偶联受体 (GPCR) 激酶 5 (GRK5) 共价抑制剂 (IC50: 220 nM)。CCG-273220 可以共价结合GRK5亚家族特异性残基 Cys474 ，而对GRK5的选择性比 GRK2 高。
T36838	(R)-Bromoenol lactone
	The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β exce...
T69632	VRT-043198
	VRT-043198 是 VX-765 (Belnacasan) 的活性代谢物，是有效的、选择性的、能透过血脑屏障的caspase-1的抑制剂。VRT-043198 对caspase-1和 caspase-4 的 Ki 值分别为 0.8 nM 和 0.6 nM。
T63405	NAZ2329
	NAZ2329 是受体型蛋白质酪氨酸磷酸酶 (RPTPs) R5 亚家族的一个细胞可渗透抑制剂，与其他 PTPs 相比，其变构且能够优先抑制 PTPRZ (hPTPRZ1 的IC50= 7.5 μM) 和PTPRG (hPTPRGIC50= 4.8 μM)。NAZ2329 能够与PTPRZ 的 D1结构域结合，与PTPRZ 整个 (D1 + D2) 片段相比，其能够更有效地抑制 PTPRZ1-D1片段 (IC50: 1.1 μM)。NAZ2329 能够抑制胶质母细胞瘤细胞的肿瘤生长，并表现出抑制干细胞样特性。
T37837	2-Methylhexacosane
	2-Methylhexacosane is a saturated hydrocarbon and an insect pheromone.1,2It has been found in the cuticle ofM. dasystomusfemales, but not males, where it contributes to the mating behavior of males, as well as inD. melanogasterfemales where it modulates aggression of males towards females. 2-methylhexacosane has also been found in yellow jacket (V. vulgaris) trail extracts.3 1.Spikes, A.E., Pashen, M.A., Millar, J.G., et al.First contact pheromone identified for a longhorned beetle (Coleoptera: ...

化合物

Cat.No: T16483

Target: TRP/TRPV Channel

TRPM4 inhibitor 8

Cat.No: T9776

Target: TRP/TRPV Channel

1,1'-Methylenedi-2-naphthol

Cat.No: T9335

Synonym: 1，1-亚甲基-2-萘酚,Squoxin

Target: Others

NR2F6 modulator-1

Cat.No: T62204

Target: Others

Cat.No: T28020

Target: TRP/TRPV Channel

Rhosin hydrochloride

Cat.No: T16745

Target: Apoptosis, Rho, Ras

Cat.No: T16763

Target: TRP/TRPV Channel

BRM/BRG1 ATP Inhibitor-1

Cat.No: T10616

Target: Epigenetic Reader Domain

Cat.No: T2024

Synonym: A 803467,A803467

Target: Sodium Channel

Cat.No: TP2158

Synonym: TRV-120027 TFA (1234510-46-3 free base)

Target: RAAS, Arrestin

Cat.No: T23429

Synonym: TC-E 5002

Target: Others

Cat.No: T70716

Cat.No: T63411

Cat.No: T68693

Cat.No: T71359

Cat.No: T82579

Cat.No: T16746

Target: Rho

Cat.No: T37086

type I hair keratin fragment [Homo sapiens]/[Ovis aries]/[Rattus norvegicus]

Cat.No: TP2188

Target: Others

Rac GTPase fragment

Cat.No: TP2287

Target: Others

Cat.No: T63340

(R)-Bromoenol lactone

Cat.No: T36838

Cat.No: T69632

Cat.No: T63405

2-Methylhexacosane

Cat.No: T37837

Cat. No.	Product Name	Target	Signaling Pathways
T3719	Daminozide Succinic Acid,DMASA,Aminozide,丁酰肼	Histone Demethylase	Chromatin/Epigenetic
	Daminozide (Succinic Acid) 是一种植物生长调节剂，选择性地抑制 KDM2/7 JmjC 亚家族，对PHF8、KDM2A 和KIAA1718的IC50值分别为 0.55、1.5 和 2.1 μM。

天然产物

Cat.No: T3719

Synonym: Succinic Acid,DMASA,Aminozide,丁酰肼

Target: Histone Demethylase

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