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61

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12692	RAS GTPase inhibitor 1	Others	Others
	RAS GTPase inhibitor 1 is a inhibitor of RAS GTPase, with anti-tumor activity.
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).
T22106	MLS-573151	CDK; Ras	Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	MLS-573151 是 GTPase Cdc42 的选择性抑制剂，EC50 为 2 μM。它通过阻止 GTP 与 Cdc42 的结合来发挥作用。
T6822	Hydroxy-Dynasore Dyngo-4a	Dynamin	Cytoskeletal Signaling
	Hydroxy-Dynasore (Dyngo-4a) 是 Dynasore 结构模拟类似物，是一种改进的，低细胞毒性的 dynamin 通用抑制剂，抑制 dynamin 依赖性转铁蛋白的内吞作用的 IC50为 5.7 μM，对大脑重组 dynamin I 和重组鼠 dynamin II 的 IC50值分别为 0.38 μM 和 2.3μM。
T7558	CID-1067700 2-[[(苯甲酰基氨基)硫代甲酰]氨基]-4,7-二氢-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸	Ras	GPCR/G Protein; MAPK
	CID-1067700 是泛 GTPase 抑制剂，可竞争性抑制大脑 7 (Rab7) 中的 Ras 相关蛋白，Ki 为 13 nM。
T3971	CASIN Pirl1-related Compound 2	CDK; STAT; Ras	Cell Cycle/Checkpoint; GPCR/G Protein; JAK/STAT signaling; MAPK; Stem Cells
	CASIN (Pirl1-related Compound 2) 是选择性GTPase Cdc42抑制剂，IC50值是 2 uM。
T1855	ZCL278 ZCL 278	CDK; Ras	Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	ZCL278 是一种选择性 Cdc42 GTPase 抑制剂，与Cdc42结合，Kd 为 11.4 μM。
T6342	NSC 23766 trihydrochloride Rac1 Inhibitor,NSC 23766	Apoptosis; Rho; Ras	Apoptosis; Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	NSC 23766 trihydrochloride (Rac1 Inhibitor) 是一种 Rac GTPase 抑制剂，靶向 GEF 对 Rac 的激活，IC50值约为 50 μM。
TP1947L	P110 TFA	Others	Others
	P110 TFA 是一种 dynamin-related protein 1 (Drp1) 抑制剂，抑制 Drp1 GTPase 活性。
T6483	EHT 1864 EHT 1864 2HCl	Rho; Ras	Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	EHT 1864 是 Rac 家族 GTPase 抑制剂，对 Rac1、Rac1b、Rac2 和 Rac3的Kd 为 40、50、60 和 250 nM。
T1848	Dynasore Dynamin Inhibitor I	Dynamin; Virus Protease; Autophagy; HSV	Autophagy; Cytoskeletal Signaling; Microbiology/Virology
	Dynasore (Dynamin Inhibitor I) 是一种可渗透细胞的化学物质，可逆且非竞争性地抑制 dynamin 1/2 的 GTPase 活性。它还抑制线粒体动力蛋白 Drp1，对其他小 GTPase 没有影响。
T21798L	Dynamin inhibitory peptide Acetate Dynamin inhibitory peptide Acetate(251634-21-6 Free base)	GTPase	GPCR/G Protein
	Dynamin inhibitory peptide Acetate 是一种具有序列 Gln-Val-Pro-Ser-Arg-Pro-Asn-Arg-Ala-Pro 的肽，可抑制 GTPase dynamin。
T2463	ML141 CID-2950007	Apoptosis; CDK; Ras	Apoptosis; Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	ML141 (CID-2950007) 是一种高效变构，选择性可逆的 Cdc42 GTPase 非竞争性抑制剂，IC50值为200 nM。它抑制 Cdc42 野生型和 Cdc42 Q61L 突变体。
T14775	Bragsin2 6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one,Bragsin 2	Others	Others
	Bragsin2 (6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one) 是非竞争性的核苷酸交换因子 BRAG2选择性抑制剂，其 IC50值为 3 μM。它能够结合到 BRAG2 的 PH 结构域和磷脂双分子层的界面处，使 BRAG2 无法激活磷脂化的 Arf GTPase。它能够影响乳腺癌干细胞。
T38387	Compound C108	GTPase	GPCR/G Protein
	Compound C108 是 GTPase 激活蛋白 SH3 结构域结合蛋白 2 (G3BP2) 的抑制剂。 Compound C108可用于乳腺肿瘤和食管鳞状细胞癌的研究。
T2427	EHop-016 EHop 016	Rho; Ras	Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	EHop-016 是一种特异性 Rac GTPase 抑制剂，对 MDA-MB-231 和 MDA-MB-435 细胞中的 Rac1 的 IC50 为 1.1 μM，也可抑制Rac3 。它还抑制 Vav2 与 Rac，Rac 激活的 PAK1 相互作用，片状脂蛋白形成和细胞迁移。
T64369	Dynamin IN-2	Dynamin	Cytoskeletal Signaling
	Dynamin IN-2是一种Wiskostatin 类似物。Dynamin IN-2有效抑制 dynamin ，对 dynamin I GTPase 的 IC50 为 1.0 μM。Dynamin IN-2 可阻断网格蛋白介导的内吞作用 (CME)，IC50 为 9.5 μM。
T22981	Tetradecyltrimethylammonium bromide MitMAB,Cetrimide,tetradecyl trimethyl ammonium bromide,十四烷基三甲基溴化铵	Dynamin	Cytoskeletal Signaling
	Tetradecyltrimethylammonium bromide (MitMAB) 是一种具有不对称结构的阳离子表面活性剂，是一种有机结构单元。
T4022	QS11 QS 11	GTPase	GPCR/G Protein
	QS11 是一种ARFGAP1抑制剂(EC50:1.5 µM)。QS 11 能抑制 ARFGAP 过表达的乳腺癌细胞迁移。QS 11 通过影响蛋白质运输来增强 Wnt/β-catenin 信号。
T25214	CCR-11 CCR11,CCR 11	Antibiotic	Microbiology/Virology
	CCR-11 是一种具有抗菌活性的绕丹宁衍生物。 CCR-11 可以抑制 B. subtilis细胞和 HeLa 细胞增殖。 CCR-11 通过抑制 FtsZ 的组装和 GTPase 活性来抑制细菌增殖和细菌胞质分裂。 CCR-11 具有潜在的抗肿瘤活性，可用于研究乳腺癌和小儿骨髓增生异常。
T79213	AZD4747	Ras	GPCR/G Protein; MAPK
	AZD4747 是一种可透过血脑屏障且具有选择性和有效性的突变GTP酶 KRAS G12C 抑制剂，具有潜在的抗肿瘤活性，可用于研究胰腺癌和结直肠腺癌。
T71740	CID-4785700 CID4785700	GTPase	GPCR/G Protein
	CID-4785700 是一种有效的泛 GTP 酶抑制剂,抑制Rab7，抑制与 Asf1 和 Vps75 结合的真菌组蛋白乙酰转移酶 Rtt109，可用于研究红斑狼疮。
T34973	Tyrphostin 8 4-Hydroxybenzylidenemalononitrile	EGFR; GTPase	Angiogenesis; GPCR/G Protein; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) 是一种有效的 GTP 酶抑制剂，对 EGFR 激酶有抑制作用， IC50 值为 560 μM。Tyrphostin 8 可抑制蛋白丝氨酸/苏氨酸钙调磷酸酶 (IC50=21 μM)，增强 Caco-2 细胞中转铁蛋白受体介导的转吞作用，并增加口服胰岛素 - 转铁蛋白的降血糖作用。
T6634	RBC8	GTPase; Ras	GPCR/G Protein; MAPK
	RBC8是一种特异性 GTP 酶 RalA/RalB 抑制剂，通过抑制 Ral 与其效应物 RALBP1 的结合，对 GTP 酶 RhoA 和 Ras 没有抑制作用。
T25529	IMM-01	GTPase	GPCR/G Protein
	IMM-01 是一类新型的哺乳动物透明 (mDia) 相关形式的小分子激动剂，其作用于 Rho GTPase 下游以组装肌动蛋白丝，并与微丝组织在迁移和不对称分裂过程中建立和维持细胞极性. GTP 结合的 Rho 通过破坏 DID 和 DAD 自动调节结构域之间的相互作用来激活 mDia 家族成员，从而释放 FH2 结构域以调节肌动蛋白和微管动力学。
T1907	Mdivi-1 Mitochondrial division inhibitor 1	Apoptosis; Mitophagy; Dynamin; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling
	Mdivi-1 (Mitochondrial division inhibitor 1) 是一种线粒体分裂抑制剂，抑制 DRP1 和 Dynamin I (IC50=1-10 μM)。Mdivi-1 可以抑制线粒体自噬。
T38407	RTIL 13
	RTIL 13 is a highly effective inhibitor of dynamin GTPase, exhibiting an IC50 value of 2.3 μM for dynamin I GTPase. Furthermore, it selectively interacts with the pleckstrin homology lipid binding domain. This compound effectively suppresses both receptor-mediated and synaptic vesicle endocytosis, demonstrating IC50 values of 9.3 μM and 7.1 μM, respectively.
T77772	MiTMAB
	MiTMAB，一种选择性动力蛋白（dynamin）抑制剂，其作用机制为靶向动力蛋白与磷脂之间的相互作用。该抑制剂能够抑制dynamin GTPase活性，Ki值为940 nM。
T35674	StRIP16
	Rab8a GTPase-binding stapled peptide (Kd = 12.7 μM). Cell permeable; localizes to the endomembrane system. Cromm et al (2016) Protease-resistant and cell-permeable double-stapled peptides targeting the Rab8a GTPase. ACS Chem.Biol. 11 2375 PMID:27336832
T27822	LFF 571 LFF571,LFF-571
	LFF 571 is an inhibitor of protein-synthesizing GTPase (Elongation Factor).
T14774	Bragsin1	Others	Others
	Bragsin1 is a potent and selective and noncompetitive ArfGEF BRAG2 inhibitor, inhibits Arf GTPase activation(IC50 : 3 μM),and with anti-cancer activity.
T68788	Ellipticine quinone
	Ellipticine quinone, also known as NSC-383230, is a Drp1 inhibitor. rpitor1 and Drpitor1a inhibited the GTPase activity of Drp1 without inhibiting the GTPase of dynamin 1. Ellipticine quinone showed greater potency than the current std. Drp1 GTPase inhibitor, mdivi-1, (IC50 for mitochondrial fragmentation are (0.06, and 10 μM, resp.). Ellipticine quinone suppressed lung cancer tumor growth in a mouse xenograft model. Ellipticine quinone also inhibited mitochondrial ROS prodn., prevented mi...
T25951	Phox-I1 Phox I1
	Phox-I1 is a NOX2 inhibitor targeting the interactive site of p67phox with Rac GTPase.
T40848	NSC 23766
	NSC 23766, a cell-permeable compound, is a reversible and specific inhibitor of Rac GTPase. Its primary application lies in the field of cancer treatment.
T36535	SEC
	SEC activates ANXA7 GTPase through the AMPK/mTORC1/STAT3 signaling pathway. It selectively induces apoptosis in cancer cells expressing high levels of ITGB4 by promoting ITGB4 nuclear translocation [1][2].
TP1907	DynaMin inhibitory peptide, myristoylated
	Cell-permeable version of dynamin inhibitory peptide, an inhibitor of the GTPase dynamin that competitively blocks binding of dynamin to amphiphysin, preventing endocytosis. Reduces NMDA receptor internalization.
T72894	Clathrin-IN-2
	Clathrin-IN-2 是网格蛋白介导的内吞作用(CME)的有效抑制剂，IC50值为 2.3 μM。 Clathrin-IN-2 还对dyn I GTPase 具有抑制作用，IC50值为 7.7 μM。
T37023	MB 0223
	Dynamin-related GTPase DRP1 partial inhibitor (IC50 = 1.2 μM). Selective for DRP1 over other dynamin-related GTPases, OPA1 and DYN1. Increases mitochondrial DNA levels in mfn1- knockout MEFs deficient in mitochondrial fusion. Mallat et al (2018) Discovery and characterization of selective small molecule inhibitors of the mammalian mitochondrial division dynamin, DRP1. Biochem.Biophys.Res.Commun. 499 556 PMID:29601815
T39857	8-Br-GTP 8-Bromoguanosine-5'-triphosphate,8-Br-GTP
	8-Br-GTP, an analog of GTP, functions as both a competitive inhibitor of FtsZ polymerization and GTPase activity (with a K i value of 31.8 μM). Moreover, it is capable of facilitating nucleic acid modification.
T63370	FtsZ-IN-2
	FtsZ-IN-2 是细菌细胞分裂蛋白 FtsZ 抑制剂，对 GTPase 的活性具有抑制作用。FtsZ-IN-2 表现出抗葡萄球菌作用，对 MSSA 和 MRSA 的MIC 值均为 2 μg/ml。
T83057	Anti-inflammatory agent 49
	Anti-inflammatory agent 49 (化合物 SC9)，一种Drp1-Fis1相互作用的抑制剂，可用于缓解Fis1介导的线粒体功能障碍。该化合物在体外对GTPase的IC50值为270 nM。
T73456	DRP1i27
	DRP1i27是一种有效抑制人源Drp1(动力蛋白相关蛋白1)的化合物。它通过与Drp1的GTPase位点结合，并与Gln34及Asp218形成氢键来发挥作用。DRP1i27主要针对Drp1介导的线粒体裂变细胞系模型，能有效防止模拟缺血再灌注引起的损伤。
TP2039	Dynamin inhibitory peptide, myristoylated (control)
	Control peptide version of dynamin inhibitory peptide, myristoylated, an inhibitor of the GTPase dynamin that competitively blocks binding of dynamin to amphiphysin, preventing endocytosis. In contrast to dynamin inhibitory peptide, has no significant eff
T35437	(-)-Viriditoxin
	(-)-Viriditoxin is a mycotoxin originally isolated from A. viridinutans that has antibacterial and antiproliferative activity. It is active against methicillin-sensitive and -resistant S. aureus (MSSA and MRSA, respectively), tetracycline-sensitive and -resistant Staphylococcus, vancomycin-sensitive and -resistant Enterococcus, and penicillin-sensitive and -resistant S. pneumoniae (MICs = 2-32 μg/ml). (-)-Viriditoxin is also active against fish pathogens, including S. iniae and S. parauberis (MI...
T35670	Miro1 Reducer
	Promotes proteasomal degradation of Miro1 (mitochondrial Rho GTPase 1). Reduces Miro1 levels in fibroblasts from Parkinson's disease (PD) patients (IC50 = 7.8 μM). Exhibits no significant effect on related outer mitochondrial membrane protein Mitofusin. Reduces stress-induced degeneration of dopaminergic neurons derived from PD patient iPSCs. Rescues age-dependent neuronal loss and prolongs lifespan in fly PD models.
TP1947	P110
	Dynamin-related protein 1 (Drp1) inhibitor, inhibits Drp1 GTPase activity. Displays no effect on dynamin 1 or other mitochondrial dynamics-related proteins. Inhibits mitochondrial fission, dysfunction and reactive oxygen species (ROS) production in vitro.
T35003	UR-PI376 UR-PI 376,UR-PI-376,URPI-376,URPI 376
	UR-PI376 is a histamine H4 receptor agonist (hH4R agonist) (pEC50 = 7.47, alpha = 0.93), with low activity for hH1R and hH2R and significant selectivity for hH3R (pKB = 6.00, alpha =- 0.28), as in stable-use a membrane preparation of hH(x)R-expressing Sf9
T29086	VA5 TG2 inhibitor VA5,VA-5,VA 5
	VA5 is an transamidase inhibitor by direct binding at the transamidase site. VA5 also inhibits GTP-binding activities. It interaction at the transamidase site locks the protein in the extended/open conformation to disorganize/inactivate the GTP binding/GT
T83814	8-Bromoguanosine-5'-O-triphosphate sodium 8-bromo GTP
	8-Bromoguanosine-5'-O-triphosphate是一种guanosine 5'-triphosphate (GTP)的衍生物，后者是蛋白质合成和糖异生作用的能量底物。该化合物在31.8 µM的浓度下抑制大肠杆菌的GTPase FtsZ（Ki = 31.8 µM），但在500 µM的浓度下，能促进在无细胞测定中猪脑微管的组装。
T81754	mP6 Myr-FEEERA-OH	Integrin	Cytoskeletal Signaling
	mP6（Myr-FEEERA-OH）为肉豆蔻酰化肽，能特异性抑制Gα13与整合素β3间相互作用，且不影响talin依赖的整合素功能。它还能阻碍Rac1、Rap1、Rab7的GTP利用，有效抑止CHO-A24细胞感染。

化合物

RAS GTPase inhibitor 1

Cat.No: T12692

Target: Others

Rac GTPase fragment

Cat.No: TP2287

Target: Others

Cat.No: T22106

Target: CDK, Ras

Hydroxy-Dynasore

Cat.No: T6822

Synonym: Dyngo-4a

Target: Dynamin

Cat.No: T7558

Synonym: 2-[[(苯甲酰基氨基)硫代甲酰]氨基]-4,7-二氢-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸

Target: Ras

Cat.No: T3971

Synonym: Pirl1-related Compound 2

Target: CDK, STAT, Ras

Cat.No: T1855

Synonym: ZCL 278

Target: CDK, Ras

NSC 23766 trihydrochloride

Cat.No: T6342

Synonym: Rac1 Inhibitor,NSC 23766

Target: Apoptosis, Rho, Ras

Cat.No: TP1947L

Target: Others

Cat.No: T6483

Synonym: EHT 1864 2HCl

Target: Rho, Ras

Cat.No: T1848

Synonym: Dynamin Inhibitor I

Target: Dynamin, Virus Protease, Autophagy, HSV

Dynamin inhibitory peptide Acetate

Cat.No: T21798L

Synonym: Dynamin inhibitory peptide Acetate(251634-21-6 Free base)

Target: GTPase

Cat.No: T2463

Synonym: CID-2950007

Target: Apoptosis, CDK, Ras

Cat.No: T14775

Synonym: 6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one,Bragsin 2

Target: Others

Cat.No: T38387

Target: GTPase

Cat.No: T2427

Synonym: EHop 016

Target: Rho, Ras

Cat.No: T64369

Target: Dynamin

Tetradecyltrimethylammonium bromide

Cat.No: T22981

Synonym: MitMAB,Cetrimide,tetradecyl trimethyl ammonium bromide,十四烷基三甲基溴化铵

Target: Dynamin

Cat.No: T4022

Synonym: QS 11

Target: GTPase

Cat.No: T25214

Synonym: CCR11,CCR 11

Target: Antibiotic

Cat.No: T79213

Target: Ras

Cat.No: T71740

Synonym: CID4785700

Target: GTPase

Cat.No: T34973

Synonym: 4-Hydroxybenzylidenemalononitrile

Target: EGFR, GTPase

Cat.No: T6634

Target: GTPase, Ras

Cat.No: T25529

Target: GTPase

Cat.No: T1907

Synonym: Mitochondrial division inhibitor 1

Target: Apoptosis, Mitophagy, Dynamin, Autophagy

Cat.No: T38407

Cat.No: T77772

Cat.No: T35674

Cat.No: T27822

Synonym: LFF571,LFF-571

Cat.No: T14774

Target: Others

Ellipticine quinone

Cat.No: T68788

Cat.No: T25951

Synonym: Phox I1

Cat.No: T40848

Cat.No: T36535

DynaMin inhibitory peptide, myristoylated

Cat.No: TP1907

Cat.No: T72894

Cat.No: T37023

Cat.No: T39857

Synonym: 8-Bromoguanosine-5'-triphosphate,8-Br-GTP

Cat.No: T63370

Anti-inflammatory agent 49

Cat.No: T83057

Cat.No: T73456

Dynamin inhibitory peptide, myristoylated (control)

Cat.No: TP2039

(-)-Viriditoxin

Cat.No: T35437

Cat.No: T35670

Cat.No: TP1947

Cat.No: T35003

Synonym: UR-PI 376,UR-PI-376,URPI-376,URPI 376

VA5 TG2 inhibitor

Cat.No: T29086

Synonym: VA5,VA-5,VA 5

8-Bromoguanosine-5'-O-triphosphate sodium

Cat.No: T83814

Synonym: 8-bromo GTP

Cat.No: T81754

Synonym: Myr-FEEERA-OH

Target: Integrin

Cat. No.	Product Name	Target	Signaling Pathways
TQ0183	Narciclasine 水仙环素,Lycoricidinol	ROCK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	Narciclasine (Lycoricidinol) 是一种植物生长调节剂。它通过调节Rho/Rho 激酶/LIM 激酶/cofilin 信号传导途径，大大增加GTP 酶RhoA 活性以及以RhoA 依赖性方式诱导肌动蛋白应力纤维形成。
T4969	Guanosine 5'-triphosphate trisodium salt 鸟苷-5'-三磷酸三钠盐,GTP Trisodium salt,5'-GTP trisodium salt	Endogenous Metabolite	Metabolism
	Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) 为G蛋白(G proteins)信号转导过程中的活化剂。
TN4098	Gancaonin I	GTPase; Antifection	GPCR/G Protein; Microbiology/Virology
	Gancaonin I exhibits anti-BsFtsZ GTPase activities; it also shows significant inhibitory activity against B. subtilis, with a MIC value of 5 uM.

天然产物

Cat.No: TQ0183

Synonym: 水仙环素,Lycoricidinol

Target: ROCK

Guanosine 5'-triphosphate trisodium salt

Cat.No: T4969

Synonym: 鸟苷-5'-三磷酸三钠盐,GTP Trisodium salt,5'-GTP trisodium salt

Target: Endogenous Metabolite

Cat.No: TN4098

Target: GTPase, Antifection

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