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43

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP2330	D-loop peptide, synthetic D-Loop protein
	D-loop peptide, synthetic is an antigenic peptide. It cyclizes through a peptide bond between the side chain carboxylic group of Asp10 and the terminal amide of the peptide.
TP1740	GroES mobile loop
	GroES mobile loop is a flexible region of unbound GroES that interacts with GroEL via the residues located at the tip of the loop.
T10441	Azosemide	Na-K-Cl cotransporter	Membrane transporter/Ion channel
	Azosemide 是磺胺类环利尿剂和NKCC1抑制剂，对 hNKCC1A 和 NKCC1B 的IC50分别为 0.246 和 0.197 µM。
TP1563	Gap19	Gap Junction Protein	Cytoskeletal Signaling
	Gap19 是一种衍生自 Cx43 细胞质环九个氨基酸的肽，是选择性连接蛋白 43 半通道阻滞剂。它可以防止 C 末端与 CL 的分子内相互作用，具有保护心肌作用。
T22461	YKL-5-124	CDK	Cell Cycle/Checkpoint
	YKL-5-124 是选择性不可逆CDK7共价抑制剂，对CDK7和CDK7/Mat1/CycH 的IC50分别为 53.5 nM 和 9.7 nM。它诱导强烈的细胞周期停滞，并抑制 E2F 驱动的基因表达。它对 CDK7 的生化和细胞选择性优于 CDK12/13。它对CDK7的选择性比 CDK9 和 CDK2 高 100 倍以上。
T20807	Looplure ENT 33266,Pherocon CL,AI3-33266,Cabblemone,(Z)-7-Dodecen-1-olacetate
	Looplure is a chemosterilant, insect attractant and repellent.
T13932	TLR1 N-[(1S)-2-甲基-1-(1-吡咯烷羰基)丙基]-苯丙酰胺	Others; MyD88	Immunology/Inflammation; Others
	TLR1 是细胞穿透 Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop 的小分子模拟物，能够阻碍 IL-1 受体介导的反应。
T1410	Torsemide AC-4464,JDL-464,托拉塞米,Torasemide	Na-K-Cl cotransporter	Membrane transporter/Ion channel
	Torsemide (AC-4464) 是具有口服活性的亨氏环利尿剂，也具有抗醛固酮和血管舒张活性。它可用于研究心力衰竭、肾脏疾病、肝硬化。
T4564	Ethacrynic acid Edecrin,利尿酸,Etacrynic Acid,Hydromedin	Others; Calcium Channel; NF-κB; GST	Membrane transporter/Ion channel; Metabolism; NF-κB; Others; oxidation-reduction
	Ethacrynic acid (Edecrin) 是谷胱甘肽 S-转移酶抑制剂，也是NF-κB 信号传导途径的有效抑制剂，并且还调节白三烯的形成。它还可抑制 L 型电压依赖性和储存操作的钙通道，从而导致气道平滑肌细胞松弛。它是利尿剂，具有抗炎特性，可减轻类维生素 A 诱导的小鼠耳部水肿。
T8705	BOT-64	IκB/IKK	NF-κB
	BOT-64 是一种 IKK-2 抑制剂，靶向激酶激活环结构域中的 Ser177 和/或 Ser181 残基。BOT-64 是一种可渗透细胞的苯并恶硫醇化合物。
TP1813L	Dynorphin A 1-10 acetate(79994-24-4 free base)	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Dynorphin A 1-10 acetate(79994-24-4 free base) 是一种内源性 opioid 样物质神经肽，与 κ-opioid 样物质受体的细胞外环 2 结合。 Dynorphin A (1-10) 还阻断 NMDA 激活的电流，IC50 为 42.0 μM。
T0114	Trichlormethiazide Naqua,Metahydrin,三氯噻嗪,Trichlormetazid	ATPase; Carbonic Anhydrase	Membrane transporter/Ion channel; Metabolism
	Trichlormethiazide (Naqua) 是一种口服具有活力的噻嗪类利尿剂，具有降压作用。它能够提高急性肾功能衰竭大鼠的尿量、Na 和 K 排泄，并有改善降低的肌酐清除率。
TP2311	C-MYC PEPTIDE EPITOPE TFA	Others	Others
	C-MYC PEPTIDE EPITOPE TFA 是 c-myc 原癌基因的产物，是一种螺旋-环-螺旋亮氨酸拉链磷蛋白，可调节细胞增殖、细胞分化和凋亡中的基因转录。该肽是人类 c-myc 表位。
T24076	FzM1 FzM 1,FzM-1	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	FzM1 是卷曲蛋白受体 FZD4 的负变构调节剂 (NAM)。 FzM1减少 WNT5A 依赖的 WNT 反应元件 (WRE) 活性 (log EC50inh=-6.2)。 FzM1 与位于 FZD4 细胞内环 3 (ICL3) 的变构结合位点结合并改变受体的构象，从而抑制 WNT/β-连环蛋白级联反应。
T13387L	Zatebradine hydrochloride UL-FS-49CL,UL-FS-49	Others; HCN Channel	Membrane transporter/Ion channel; Others
	Zatebradine hydrochloride (UL-FS-49CL) 是一种高效的、有效的HCN Channel 抑制剂( IC50 ：1.96 µM)。 HCN Channel 是一种有效的超极化激活环核苷酸门控通道。 Zatebradine hydrochloride 阻止通过人类 HCN1，HCN2，HCN3 和 HCN4 通道的缓慢内向电流，其 IC50 值分别为 1.83 µM，2.21 µM，1.90 µM 和 1.88 µM。
T35336	Furosemide sodium Frusemide Sodium,Lasix	Na-K-Cl cotransporter	Membrane transporter/Ion channel
	Furosemide sodium (Frusemide Sodium) 是 Na+/K+/2Cl- (NKCC)，NKCC1 和 NKCC2 共转运蛋白的有效的和具有口服活性抑制剂。Furosemide sodium 也是 GABAA 受体拮抗剂，对含 α6 受体的选择性是含 α1 受体的 100 倍。Furosemide sodium 用作利尿试剂，用于充血性心力衰竭，高血压和水肿的研究。
T10936	D-I03 DI03	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	D-I03 是一种选择性的RAD52 抑制剂，Kd 为 25.8 µM。D-I03 抑制 RAD52 依赖性单链退火 (SSA) 和 D 环形成，IC50 分别为 5 µM 和 8 µM。D-I03 抑制 BRCA1 和 BRCA2 缺陷细胞的生长，并抑制顺铂诱导的 RAD52 病灶形成，但对 RAD51 无影响。
T33851	Ozolinone W 3282,W3282,W-3282
	Ozolinone is an active metabolite of etozoline which acts as a loop diuretic --- a diuretic that acts at the ascending limb of the loop of Henle in the kidney. Loop diuretics are primarily used in medicine to treat hypertension and edema often due to cong
T19788	Piretanide Eurelix,Tauliz,Arelix
	Piretanide is a time- and voltage-dependent blocker of CFTR Cl(-) currents. Piretanide also acts as a loop diuretic.
T30590	Brocrinat HP 522
	Brocrinat (HP 522) is an active diuretic with at least one site of action in the medulla oblongata branch of the Henle loop.
T68607	AP23848
	AP23848 is a potent Bcr-Abl inhibitor. In a murine model, AP23848 inhibited activation-loop mutant Kit phosphorylation and tumor growth.
T18527	PDdB-Pfp	Others	Others
	PDdB-Pfp is a reducible ADC (antibody-drug conjugate) linker designed for agents targeting the extracellular loop 1 (ECL1) of TM4SF1 (transmembrane 4 L6 family member 1).
TP1813	Dynorphin A (1-10) Dynorphin A 1-10
	Dynorphin A (1-10), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
T68581	AP23464
	AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the lo...
T33432	MK-3281 MK 3281,MK3281
	MK-3281 is a potent, orally bioavailable hepatitis C virus NS5B polymerase finger-loop inhibitor. It is also an inhibitor of attractive molecular properties with good potency in HCV subgenomic replication trials and suitable for clinical candidates.
T19849	2-PADQZ 2PADQZ,2-PADQZ
	DPQ is an antiviral compound. DPQ has also been shown to bind to a widened RNA major groove at the internal loop. DPQ acts against the H1N1 and H3N2 strains of influenza A as well as influenza B.
T18531	PDP-Pfp	Others	Others
	PDP-Pfp is a reducible ADC linker primarily utilized for targeting agents aimed at the extracellular loop 1 (ECL1) of TM4SF1, a member of the transmembrane 4 L6 family, as supported by reference [1].
T28536	RI(dl)-2 TFA RI(dl)-2
	RI(dl)-2 TFA 是一种有效的选择性 RAD51 介导的 D 环形成 (RAD51-mediated D-loop formation) 抑制剂，IC50为 11.1 μM，并抑制人细胞中的同源重组 (HR) 活性，IC50为 3.0 μM。
T61713	Bumetanide sodium
	Bumetanide sodium is a potent loop diuretic that acts as a blocker for the sodium-potassium-chloride cotransporter (NKCC). It selectively inhibits NKCC1 and NKCC2, with IC50 values of 0.68 μM and 4.0 μM for hNKCC1A and hNKCC2A, respectively [1] [2].
T72001	CB096
	CB096 is a novel inhibitor of RAN translation. specifically binds to a repeating 1 × 1 GG internal loop structure, 5'CGG/3'GGC, that is formed when r(G4C2)exp folds, also acting as a potent vasorelaxant agent, showing antihypertensive effect.
T80580	Zinlirvimab 10-1074
	Zinlirvimab是一种IgG1-λ2类人源化HIV中和抗体，专一性靶向HIV-1 gp120包膜糖蛋白(IIIB gp120 V3环)。
T75988	Dynorphin A (1-10) (TFA)
	Dynorphin A (1-10) (TFA) 是一种内源性的阿片样神经肽，与 κ 阿片受体 (κ-opioid receptor) 结合。Dynorphin A (1-10) (TFA) 也阻断 NMDA 激活的电流，IC50为 42.0 μM。
T75795	Gap 26 TFA
	Gap 26 TFA 是一种连接蛋白 (connexin) 模拟肽，由连接蛋白 connexin 43 (gap junction 阻滞剂)一个胞外环的第 63-75 残基组成，包含SHVR 氨基酸基序。
T62355	HBV-IN-14
	HBV-IN-14 是一种吡啶并嘧啶酮类化合物，也是一种有效的共价闭合环状 DNA (cccDNA) 抑制剂。其中 cccDNA 是一种病毒 RNA 转录和随后病毒 DNA 生成的模板。HBV-IN-14 具有潜力进行 HBV 感染的研究。
T71586	Z-VAE(OMe)-fmk
	Z-VAE(OMe)-fmk is a cell-permeable and irreversible UCHL1 inhibitor. The inhibitor approaches the active-site cleft from the opposite side of the crossover loop as compared to the direction of approach of ubiquitin's C-terminal tail, thereby occupying the P1' (leaving group) site, a binding site perhaps used by the unknown C-terminal extension of ubiquitin in the actual in vivo substrate(s) of UCHL1.
T39459	THZ-P1-2 THZ-P1-2
	THZ-P1-2 is a novel, specific inhibitor of PI5P4K that effectively targets PI5P4Kα. With an IC 50 of 190 nM, THZ-P1-2 selectively inhibits PI5P4Kα by forming covalent bonds with cysteine residues located on a disordered loop present in PI5P4Kα/β/γ. This mechanism not only disrupts autophagy but also elevates TFEB signaling. Moreover, THZ-P1-2 exhibits potent anticancer effects in leukemia cell lines, making it a promising candidate for therapeutic applications.
T36127	TNF-α Antagonist
	TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destr...
T82683	Connexin mimetic peptide 40GAP27
	Connexin mimetic peptide 40GAP27 是一种生物活性肽，对应于主要的血管连接蛋白Cx40第二个细胞外环的GAP27结构域（40Gap27）。该化合物在研究氧化应激所致的损伤以及间隙连接通讯机制中有应用。40Gap27能够在给药后减少内皮依赖性的内膜下平滑肌的超极化现象。
TP1581	C-Type Natriuretic Peptide (1-53), human
	CNP, a member of the natriuretic peptide family, was first identified in porcine brain and later found in other mammals as well as non-mammals. Processing of the CNP precursor gives rise to CNP-22 and its N-terminally elongated form, CNP-53. The CNPs shar
T75820	Gap19 TFA
	Gap19 TFA，源自Cx43胞浆环(CL)的九个氨基酸肽，是高效且选择性的连接蛋白43 (Cx43) 半通道阻滞剂。该肽阻止C末端（CT）与CL之间的分子内相互作用，但不影响GJ通道或Cx40/pannexin-1半通道。此外，Gap19 TFA对心肌有保护作用。
T68525	Nafarelin acetate hydrate
	Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. Nafarelin increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of estrogen/progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will negatively feed back upon hypothalamus to decrease GnRH ( negative feedback loop ) Through negative feedback, Nafarelin causes a decrease in pituitary secretion of gonadotropins lu...
T82684	Connexin mimetic peptide 40,37GAP26
	Connexin mimetic peptide 40,37GAP26是一种生物活性肽，对应Cx37和Cx40主要血管连接蛋白的胞外环GAP26结构域，命名基于Cx同源性为37,40Gap26。本化合物主要用于研究间隙连接对环吡嗪酸(CPA)通过啮齿动物髂动脉壁导致的内皮超极化扩散的影响。Cx37和Cx40形成的间隙连接斑块在内皮细胞中高度丰富，而Connexin mimetic peptide 40,37GAP26能抑制内膜下超极化。
T69200	CGP74514A
	CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and...

化合物

D-loop peptide, synthetic

Cat.No: TP2330

Synonym: D-Loop protein

GroES mobile loop

Cat.No: TP1740

Cat.No: T10441

Target: Na-K-Cl cotransporter

Cat.No: TP1563

Target: Gap Junction Protein

Cat.No: T22461

Target: CDK

Cat.No: T20807

Synonym: ENT 33266,Pherocon CL,AI3-33266,Cabblemone,(Z)-7-Dodecen-1-olacetate

Cat.No: T13932

Synonym: N-[(1S)-2-甲基-1-(1-吡咯烷羰基)丙基]-苯丙酰胺

Target: Others, MyD88

Cat.No: T1410

Synonym: AC-4464,JDL-464,托拉塞米,Torasemide

Target: Na-K-Cl cotransporter

Ethacrynic acid

Cat.No: T4564

Synonym: Edecrin,利尿酸,Etacrynic Acid,Hydromedin

Target: Others, Calcium Channel, NF-κB, GST

Cat.No: T8705

Target: IκB/IKK

Dynorphin A 1-10 acetate(79994-24-4 free base)

Cat.No: TP1813L

Target: Opioid Receptor

Trichlormethiazide

Cat.No: T0114

Synonym: Naqua,Metahydrin,三氯噻嗪,Trichlormetazid

Target: ATPase, Carbonic Anhydrase

C-MYC PEPTIDE EPITOPE TFA

Cat.No: TP2311

Target: Others

Cat.No: T24076

Synonym: FzM 1,FzM-1

Target: Wnt/beta-catenin

Zatebradine hydrochloride

Cat.No: T13387L

Synonym: UL-FS-49CL,UL-FS-49

Target: Others, HCN Channel

Furosemide sodium

Cat.No: T35336

Synonym: Frusemide Sodium,Lasix

Target: Na-K-Cl cotransporter

Cat.No: T10936

Synonym: DI03

Target: DNA/RNA Synthesis

Cat.No: T33851

Synonym: W 3282,W3282,W-3282

Cat.No: T19788

Synonym: Eurelix,Tauliz,Arelix

Cat.No: T30590

Synonym: HP 522

Cat.No: T68607

Cat.No: T18527

Target: Others

Dynorphin A (1-10)

Cat.No: TP1813

Synonym: Dynorphin A 1-10

Cat.No: T68581

Cat.No: T33432

Synonym: MK 3281,MK3281

Cat.No: T19849

Synonym: 2PADQZ,2-PADQZ

Cat.No: T18531

Target: Others

Cat.No: T28536

Synonym: RI(dl)-2

Bumetanide sodium

Cat.No: T61713

Cat.No: T72001

Cat.No: T80580

Synonym: 10-1074

Dynorphin A (1-10) (TFA)

Cat.No: T75988

Cat.No: T75795

Cat.No: T62355

Cat.No: T71586

Cat.No: T39459

Synonym: THZ-P1-2

TNF-α Antagonist

Cat.No: T36127

Connexin mimetic peptide 40GAP27

Cat.No: T82683

C-Type Natriuretic Peptide (1-53), human

Cat.No: TP1581

Cat.No: T75820

Nafarelin acetate hydrate

Cat.No: T68525

Connexin mimetic peptide 40,37GAP26

Cat.No: T82684

Cat.No: T69200

Cat. No.	Product Name	Target	Signaling Pathways
T3862	Irigenin	NF-κB; Integrin	Cytoskeletal Signaling; NF-κB
	Irigenin 可通过特异性和选择性地阻断 Extra Domain A 域的 C-C 环上α9β1和α4β1整合素结合位点，介导其抗转移作用。可通过增强胃癌细胞中促凋亡分子的表达来敏化 TRAIL 诱导的凋亡，具有抗癌作用。
T19146	5,6-Dihydrouridine	Endogenous Metabolite	Metabolism
	5,6-Dihydrouridine 是一种修饰碱基，存在于真核生物、细菌和某些古细菌tRNA D 环的保守位置。
T72208	1-Dehydro-[10]-gingerdione
	1-Dehydro-[10]-gingerdione 通过靶向IKKβ的激活环直接抑制 IKKβ 活性，从而破坏用激动剂刺激的巨噬细胞中 IKKβ 催化的 IκBα 磷酸化。1-Dehydro-[10]-gingerdione 抑制 LPS 诱导的NF-κB 转录活性。1-Dehydro-[10]-gingerdione 具有用于NF-κB 相关炎症和自身免疫性疾病研究的潜力。

天然产物

Cat.No: T3862

Target: NF-κB, Integrin

5,6-Dihydrouridine

Cat.No: T19146

Target: Endogenous Metabolite

1-Dehydro-[10]-gingerdione

Cat.No: T72208

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