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58

抑制剂 & 化合物

10

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6668	SGC-CBP30	Epigenetic Reader Domain; Histone Acetyltransferase	Chromatin/Epigenetic
	SGC-CBP30 是高选择性CBP/p300溴结构域的有效抑制剂，对CBP 和p300的Kd 值分别为 21 和 32 nM。它强烈减少 Th17 细胞中 IL-17A 的分泌，具有抗炎作用。
T5169	SGC-GAK-1	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	SGC-GAK-1 是细胞周期蛋白 G 相关激酶 (GAK) 的选择性抑制剂(Ki:3.1 nM)，可用作 GAK 的化学探针。
T12885	SGC-AAK1-1	AAK1 (AP2 associated kinase 1)	Neuroscience
	SGC-AAK1-1 是选择性的 AAK1(AP2 相关的激酶 1) 抑制剂，IC50=270 nM，Ki=9 nM，也抑制 BMP2K。它用于与 AAK1 相关的 Wnt 途径的研究。
T9568	SGC-SMARCA-BRDVIII	Epigenetic Reader Domain	Chromatin/Epigenetic
	SGC-SMARCA-BRDVIII 是SMARCA2/4和PB1(5)选择性抑制剂，其Kd 值分别为 35 nM，36 nM 和 13 nM。它还抑制PB1(2)和PB1(3)，Kd 值分别为 3.7 和 2.0 μM。它可阻断 3T3-L1 鼠成纤维细胞的脂肪生成。
T3084	SGC707	Histone Methyltransferase	Chromatin/Epigenetic
	SGC707 是 PRMT3化学探针，是一种有效的、选择性的、细胞活性的 PRMT3 变构抑制剂，IC50值为 31 nM。
T40131	SGC-CK2-1 SGC-CK2-1
	SGC-CK2-1 is an ATP-competitive chemical compound that acts as a highly potent and cell-active CK2 inhibitor. It demonstrates excellent selectivity towards both isoforms of human CK2, with IC50 values of 36 nM for CK2α and 16 nM for CK2α′ in the nanoBRET assay. Given its properties, SGC-CK2-1 is a suitable tool for the investigation of neurodegenerative diseases.
T7089	SGC2085	Histone Methyltransferase	Chromatin/Epigenetic
	SGC2085是一种高效选择性CARM1抑制剂，IC50值为50 nM。
T34630	SGC-AAK1-1N SGCAAK11N,SGCAAK1-1N,SGC-AAK11N
	SGC-AAK1-1N 是一种有效且选择性的 AAK1(AP2 相关激酶 1)小分子抑制剂(IC50=1.8 μM)。
T34631	SGC-GAK-1N SGC-GAK1N,SGCGAK1N,SGCGAK-1N
	SGC-GAK-1N is a negative control for SGC-GAK-1.
T3082	SGC0946	Histone Methyltransferase	Chromatin/Epigenetic
	SGC0946是一种组蛋白甲基转移酶DOT1L 高选择性抑制剂，IC50值为0.3nM，可选择性地杀死混合谱系白血病细胞。
T36976	SGC 6870
	Potent and selective protein arginine methyltransferase 6 (PRMT6) inhibitor (IC50 = 77 nM). Exhibits selectivity over all other PRMTs and 23 methyltransferases. In HEK293T cells overexpressing PRMT6, inhibits asymmetric dimethylation of H3R2 (IC50 = 0.8 μM) Negative control SGC 6870N (Cat. No. 7184) also available.
T12886	SGC-iMLLT	Histone Methyltransferase	Chromatin/Epigenetic
	SGC-iMLLT 是一种选择性的MLLT1/3-组蛋白相互作用抑制剂，IC50值为 0.26 μM，也是化学探针。它对 MLLT1 YEATS 域 (YD) 和 MLLT3 YD (AF9/YEATS3) 具有高结合力，Kd 值分别为 0.129 和 0.077 μM。
T37467	SGC 6870N
	Negative control for SGC 6870 (Cat. No. 7182). SGC 6870N is the (S)-enantiomer, which is inactive on PRMT6.
T4013	SGC2085 HCl	Histone Methyltransferase	Chromatin/Epigenetic
	SGC2085 HCl 是一种有效的选择性辅激活剂相关的精氨酸甲基转移酶 1 (CARM1) 抑制剂，IC50 为 50 nM，选择性比其他 PRMT 高出数倍。 CARM1 是结直肠癌中 Wnt/β-catenin 转录和肿瘤转化的重要正调节因子，也是雌激素刺激的乳腺癌生长的关键因素，其耗竭导致体内髓性白血病细胞增殖减少。
T69551	SGC-STK17B-1
	SGC-STK17B-1 is a potent and selective inhibitor of STK17B/DRAK2 kinase.
T34629	SGC3027N SGC-3027N,SGC 3027N
	SGC3027N is a negative control for SGC3027 (GLXC-12451).
T79542	SGC-UBD253	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SGC-UBD253为有效的HDAC6-UBD拮抗剂，常应用于癌症研究领域。
T69580	SGC6870
	SGC6870 is a novel potent, selective, and cell-active inhibitor of PRMT6 with IC50 of 77 ± 6 nM, being selective over all other PRMTs and 23 methyltransferases.
T62909	SGC agonist 2
	SGC agonist 2 是一种有效的可溶性鸟苷酸环化酶 (SGC) 激动剂。其中可溶性鸟苷酸环化酶是 NO-sGC-cGMP 信号通路中的关键信号转导酶。SGC agonist 2 具有潜力进行心血管疾病 (心力衰竭、心绞痛、肺动脉高压、心肌梗塞) 和纤维化疾病 (肾纤维化、系统性硬化症) 的研究。
T62471	SGC agonist 1
	SGC agonist 1 是一种有效的可溶性鸟苷酸环化酶 (SGC) 激动剂。SGC agonist 1 能够提高溶解度并具有高细胞通透性。SGC agonist 1 具有潜力进行心血管疾病的研究。
T7900	BAY-474	c-Met/HGFR	Tyrosine Kinase/Adaptors
	BAY-474 是酪氨酸蛋白激酶 c-MET 抑制剂，能够用于表观遗传学探针。
T21712	BAY 41-8543	Others; Guanylate cyclase	GPCR/G Protein; Others
	BAY 41-8543 是一种不依赖一氧化氮的可溶性鸟苷酸环化酶 (sGC) 刺激剂，具有抗血小板作用。它在大鼠的肺和全身血管床中具有血管舒张活性，有用于心血管疾病的研究潜力。
T12887	SGC3027	Others	Others
	SGC3027 is an inhibitor of histone methyltransferase,also is a first potent, selective and cell active chemical probe for PRMT7.
T21607	Ataciguat HMR-1766	Others; Guanylate cyclase	GPCR/G Protein; Others
	Ataciguat (HMR-1766) 是一种不依赖一氧化氮的可溶性鸟苷酸环化酶 (sGC) 激活剂，具有血管舒张作用。它能够激活 sGC 的铁血红素铁氧化还原形式，刺激 cGMP 的产生。
T12670	(Rac)-MGV354 MGV354,外消旋MGV354	Others	Others
	(Rac)-MGV354 (MGV354) 是 MGV354 的外消旋体，MGV354 是可溶性鸟苷酸环化酶活化剂，在 GTM-3E 和 CHO 细胞中 EC50分别为 5 nM 和小于 0.5 nM。
T0942	Quinacrine dihydrochloride 疟疾平,Mepacrine dihydrochloride,阿的平,SN-390,Quinacrine 2HCl	Apoptosis; Mitophagy; DNA; Phospholipase; Parasite; Autophagy; Histamine Receptor	Apoptosis; Autophagy; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience
	Quinacrine dihydrochloride (Mepacrine dihydrochloride) 是一种具有口服活性的抗疟剂，抑制 NF-κB 并激活 p53 信号转导，诱导肿瘤细胞发生凋亡，具有抗肿瘤和抗寄生虫活性。
T0006	Methylene Blue trihydrate 碱性亚甲蓝三水合物,Methylthionine chloride,Basic blue 9,亚甲蓝三水合物,Methylene Blue	Guanylate cyclase; Microtubule Associated; NO Synthase; Parasite; Monoamine Oxidase	Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience
	Methylene Blue trihydrate (Basic blue 9) 是鸟苷酸环化酶，单胺氧化酶 A 和 NO 合酶抑制剂。它是血管加压药，在医疗中通常用作染料。它具有抗伤害感受，抗疟疾，抗抑郁和抗焦虑作用，可用于高铁血红蛋白血症，神经退行性疾病和异环磷酰胺引起的脑病的研究。
T5858	Sertindole Lu 23-174,舍吲哚	Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy	Autophagy; GPCR/G Protein; Neuroscience
	Sertindole (Lu 23-174) 是一种非典型抗精神病药，可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合，Kd 值分别为 2.7、20、0.14 和 6 nM。
T7201	Nelociguat N-[4,6-二氨基-2-[1-[(2-氟苯基)甲基]-1H-吡唑并[3,4-B]吡啶-3-基]-5-嘧啶]-氨基甲酸甲酯,BAY60-4552	Guanylate cyclase	GPCR/G Protein
	Nelociguat (BAY60-4552) 是一种一氧化氮敏感的可溶性鸟苷酸环化酶刺激剂。
T16569	Praliciguat IW-1973	Others; Guanylate cyclase	GPCR/G Protein; Others
	Praliciguat (IW-1973) 是一种有效且具有口服活性的可溶性鸟苷酸环化酶 (sGC) 刺激剂，还增强 NO 信号传导，可作为血管扩张剂。在 HEK-293 细胞中，它能够刺激 sGC，EC50值为 197 nM。
T19777	ODQ	Apoptosis; Others; Guanylate cyclase	Apoptosis; GPCR/G Protein; Others
	ODQ 是一种选择性可溶性的鸟苷酰环化酶抑制剂，可增强顺铂促人间皮瘤细胞凋亡的作用。
T16383	Olinciguat IW-1701	Guanylate cyclase	GPCR/G Protein
	Olinciguat (IW-1701) 是一种口服鸟苷酸环化酶 (sGC) 刺激剂，在纯化的大鼠和人类酶测定以及全细胞测定中对 sGC 具有浓度依赖性刺激作用。
T4381	Lificiguat 利非西呱,YC-1	Others; Guanylate cyclase; HIF	Angiogenesis; Chromatin/Epigenetic; GPCR/G Protein; Others
	Lificiguat (YC-1) 是一种不依赖一氧化氮的可溶性鸟苷酸环化酶激活剂和低氧诱导因子 1α 的抑制剂。
T6775	BAY 41-2272	Guanylate cyclase	GPCR/G Protein
	BAY 41-2272 是一种直接且不依赖一氧化氮的可溶性鸟苷酸环化酶刺激剂。
T77729	MY-1076	Apoptosis; YAP	Apoptosis; Stem Cells
	MY-1076 是一种高效的 YAP 抑制剂，具有抗胃癌活性。MY-1076 剂量依赖性诱导G2/M期阻滞，诱导 YAP 降解和细胞凋亡，抑制微管蛋白聚合。MY-1076 抑制 MGC-803、SGC-7901、HCT-116 和 KYSE450 细胞增殖。
T16344	NS-2028	Others; Guanylate cyclase	GPCR/G Protein; Others
	NS-2028 是一种高度选择性的可溶性鸟苷酸环化酶抑制剂。它抑制 3-吗啉代-sydnonimine 在人培养的脐静脉内皮细胞中形成环状 GMP，IC50为30mM。它抑制小鼠小脑匀浆和神经元 NO 合酶中的可溶性鸟苷酸环化酶活性，IC50分别为 17 和 20 mM。它可降低血管内皮生长因子诱导的血管生成和通透性。
T10473	BAY-678	Others	Others
	BAY-678是一种人中性粒细胞弹性蛋白酶（HNE；IC50：20 nM）抑制剂，具有口服生物活性、高效性和选择性。BAY-678 是被基因结构组学联盟 (SGC) 推荐的化学探针。
T1984	Cinaciguat BAY 58-2667	Guanylate cyclase	GPCR/G Protein
	Cinaciguat (BAY 58-2667) 是一种不依赖于一氧化氮的鸟苷酸环化酶化剂，Kd 值为3.2 nM，可用于急性失代偿性心力衰竭的研究。
T8506	THPP-1	PDE	Metabolism
	THPP-1 是一种 SGC 推荐的化学探针，是一种口服具有活性的磷酸二酯酶10A 抑制剂，其对人和大鼠的Ki 分别为 1 nM 和 1.3 nM。它的药理学特性良好。
T10471	BAY 60-2770	Others	Others
	BAY 60-2770 is a selective and orally active soluble guanylyl cyclase (sGC) activator with antifibrotic effect. It increases the activity of sGC in a nitric oxide-independent manner.
T12661	(Rac)-BI 703704	Others	Others
	(Rac)-BI 703704 is a potent activator of soluble guanylyl cyclase (sGC).
T36981	GSK 591 dihydrochloride
	Potent and selective PRMT5 inhibitor (IC50 = 4 nM). Selective for PRMT5 over a panel of other PRMTs and lysine methyltransferases. Inhibits proliferation of mantle cell lymphoma (MCL) in vitro. To request the negative control for GSK 591, please fill out the SGC 2096 request form on the SGC website.
T69543	CFM-1571(free base)
	CFM 1571 is the free base of CFM 1571 Hydrochloride (C291720), which acts as a soluble guanylyl cyclase (sGC) activator while ignoring adenylyl cyclase.
T12888	MGV354	Others	Others
	MGV354 是一种可溶性鸟苷酸环化酶 (sGC) 激活剂，在 CHO 和 GTM-3E 细胞中 EC50值分别为 <0.5 nM 和 5 nM。
T10536	BI 703704	Others	Others
	BI 703704 是一种有效的可溶性鸟苷酸环化酶(sGC)激活剂，可抑制 ZSF1 大鼠的糖尿病肾病的进展。
T62971	Tubulin polymerization-IN-16
	Tubulin aggregation-IN-16 (compound 5g) 是一种有效的 tubulin 聚合抑制剂。Tubulin aggregation-IN-16 对癌细胞有效 (IC50: 0.084-0.221 μM)。Tubulin aggregation-IN-16 能有效地破坏微管/管蛋白的动态，诱导 SGC-7901 细胞的细胞周期阻滞在 G2/M 期。
T32242	IWP-051 IWP051
	IWP-051 is a potent, orally active sGC stimulator (EC50 = 290nM). IWP-051 showed >99% plasma protein binding, high metabolic stability, high permeability, and no efflux in a Caco-2 model of intestinal absorption. IWP-051 achieves good alignment of pote
T73332	BI-685509
	BI-685509 是一种口服有效的sGC 激活剂。BI-685509 可恢复环磷酸鸟苷 (cGMP) 并改善一氧化氮 (NO) 通路的功能。BI-685509 可用于慢性肾病 (CKD) 和糖尿病肾病 (DKD) 的研究。
T10473L	BAY-677	Others	Others
	BAY-677, serving as an inactive control for BAY-678, is distinguished by BAY-678's capabilities as an orally bioavailable, selective, and cell-permeable inhibitor of human neutrophil elastase (HNE), showcasing a high potency with an IC50 of 20 nM[1]. Furthermore, BAY-678 has been publicly nominated as a chemical probe by the Structural Genomics Consortium (SGC)[2].
T62040	Tubulin polymerization-IN-30
	Tubulin polymerization-IN-30 (compound 6e) 是有效的微管蛋白聚合 (Tubulin polymerization) 抑制剂，可破坏细胞内微管组织，将细胞周期阻滞在 G2/M 期。Tubulin polymerization-IN-30 对 HeLa、SGC-7901和A549 等肿瘤细胞系具有良好的抗肿瘤活性，其IC50分别为 0.403、 2.16和2.21 μM。

化合物

Cat.No: T6668

Target: Epigenetic Reader Domain, Histone Acetyltransferase

Cat.No: T5169

Target: Serine/threonin kinase

Cat.No: T12885

Target: AAK1 (AP2 associated kinase 1)

SGC-SMARCA-BRDVIII

Cat.No: T9568

Target: Epigenetic Reader Domain

Cat.No: T3084

Target: Histone Methyltransferase

Cat.No: T40131

Synonym: SGC-CK2-1

Cat.No: T7089

Target: Histone Methyltransferase

Cat.No: T34630

Synonym: SGCAAK11N,SGCAAK1-1N,SGC-AAK11N

Cat.No: T34631

Synonym: SGC-GAK1N,SGCGAK1N,SGCGAK-1N

Cat.No: T3082

Target: Histone Methyltransferase

Cat.No: T36976

Cat.No: T12886

Target: Histone Methyltransferase

Cat.No: T37467

Cat.No: T4013

Target: Histone Methyltransferase

Cat.No: T69551

Cat.No: T34629

Synonym: SGC-3027N,SGC 3027N

Cat.No: T79542

Target: HDAC

Cat.No: T69580

SGC agonist 2

Cat.No: T62909

SGC agonist 1

Cat.No: T62471

Cat.No: T7900

Target: c-Met/HGFR

Cat.No: T21712

Target: Others, Guanylate cyclase

Cat.No: T12887

Target: Others

Cat.No: T21607

Synonym: HMR-1766

Target: Others, Guanylate cyclase

Cat.No: T12670

Synonym: MGV354,外消旋MGV354

Target: Others

Quinacrine dihydrochloride

Cat.No: T0942

Synonym: 疟疾平,Mepacrine dihydrochloride,阿的平,SN-390,Quinacrine 2HCl

Target: Apoptosis, Mitophagy, DNA, Phospholipase, Parasite, Autophagy, Histamine Receptor

Methylene Blue trihydrate

Cat.No: T0006

Synonym: 碱性亚甲蓝三水合物,Methylthionine chloride,Basic blue 9,亚甲蓝三水合物,Methylene Blue

Target: Guanylate cyclase, Microtubule Associated, NO Synthase, Parasite, Monoamine Oxidase

Cat.No: T5858

Synonym: Lu 23-174,舍吲哚

Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Autophagy

Cat.No: T7201

Synonym: N-[4,6-二氨基-2-[1-[(2-氟苯基)甲基]-1H-吡唑并[3,4-B]吡啶-3-基]-5-嘧啶]-氨基甲酸甲酯,BAY60-4552

Target: Guanylate cyclase

Cat.No: T16569

Synonym: IW-1973

Target: Others, Guanylate cyclase

Cat.No: T19777

Target: Apoptosis, Others, Guanylate cyclase

Cat.No: T16383

Synonym: IW-1701

Target: Guanylate cyclase

Cat.No: T4381

Synonym: 利非西呱,YC-1

Target: Others, Guanylate cyclase, HIF

Cat.No: T6775

Target: Guanylate cyclase

Cat.No: T77729

Target: Apoptosis, YAP

Cat.No: T16344

Target: Others, Guanylate cyclase

Cat.No: T10473

Target: Others

Cat.No: T1984

Synonym: BAY 58-2667

Target: Guanylate cyclase

Cat.No: T8506

Target: PDE

Cat.No: T10471

Target: Others

(Rac)-BI 703704

Cat.No: T12661

Target: Others

GSK 591 dihydrochloride

Cat.No: T36981

CFM-1571(free base)

Cat.No: T69543

Cat.No: T12888

Target: Others

Cat.No: T10536

Target: Others

Tubulin polymerization-IN-16

Cat.No: T62971

Cat.No: T32242

Synonym: IWP051

Cat.No: T73332

Cat.No: T10473L

Target: Others

Tubulin polymerization-IN-30

Cat.No: T62040

Cat. No.	Product Name	Target	Signaling Pathways
TN2755	2-Desoxy-4-epi-pulchellin	Anti-infection	Microbiology/Virology
	2-Desoxy-4-epi-pulchellin 是分离自 Polygonum hydropiper 的二氯甲烷可溶部分的一种化合物。
T3S2312	Poncirin 枸橘苷,Isosakuranetin-7-neohesperidoside	Apoptosis; Others	Apoptosis; Others
	Poncirin (Isosakuranetin-7-neohesperidoside) 是从三叶草中分离出来的一种天然产物，具有抗炎活性。它防止脂肪生成，增强间充质干细胞中的成骨细胞分化，增加骨矿物质密度，改善小梁微结构，可能反映 GIO 小鼠的骨形成增加和骨吸收减少。
T3S2344	β,β-Dimethylacrylshikonin β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin	ERK; HIF/HIF Prolyl-Hydroxylase	Chromatin/Epigenetic; MAPK; Metabolism
	β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) 是一种萘醌衍生物，从 Arnebia nobilis 中提取得到。它利用 PI3K 通路诱导 eNOS、VEGF 和 HIF-1α 的表达，促进血管生成，具有抗肿瘤活性。
T75451	Cytoglobosin C
	Cytoglobosin C, 作为一种细胞松弛素衍生物，对SGC-7901和A549细胞系展现出显著的细胞毒性，IC50值均小于10 μM。
TN4960	Schleicheol 1	Others	Others
	Schleicheol 1 has antitumor activity, it possesses inhibitory activity against SGC-7901 cell line.
TN3740	Cyclocommunol	PAFR	GPCR/G Protein
	Cyclocommunol exhibits cytotoxicity against hepatocellular carcinoma (SMMC-7721) and gastric carcinoma (BGC-823 and SGC-7901) cell lines. It also shows strong inhibition of arachidonic acid (AA)- and collagen-induced platelet aggregation.
TN3429	Aphagranin A	Others	Others
	Aphagranin A exhibits strong antiproliferative activity against the growth of six lines of human cancer cells (MCF-7, A549, HepG2, Bel-7402, SGC-7901, and BGC-823.
TN4340	Ivangustin	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Ivangustin exhibits remarkable cytotoxicity against HEp2, SGC-7901 and HCT116 human cancer cell lines.
TN4239	Hydroxytanshinone IIA	Others	Others
	Hydroxytanshinone ⅡA has good antiproliferative effect on SGC-7901,HeLa, and HepG 2 cell, the values of IC50 are 4.18, 6.08 and10.20 uM, respectively; it has tumor cell proliferation inhibition significantly stronger than the tanshinoneⅡA.
TN5264	Xanthoxyletin	TNF; NOS; ROS; COX; Antifection	Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience
	Xanthoxyletin shows potent antibacterial, fungicidal, and algicidal properties, it also has anticancer, and anti-inflammatory activities. It shows an inhibitory effect on iNOS protein expression at 10 microM, it also can inhibit the synthesis of nitric oxide and the protein expression of tumor necrosis factor-alpha and cyclooxygenase-2. Xanthoxyletin induces S phase arrest and apoptosis in human gastric adenocarcinoma SGC-7901 cells, the effects are associated with the DNA damage, apoptosis thro...

天然产物

2-Desoxy-4-epi-pulchellin

Cat.No: TN2755

Target: Anti-infection

Cat.No: T3S2312

Synonym: 枸橘苷,Isosakuranetin-7-neohesperidoside

Target: Apoptosis, Others

β,β-Dimethylacrylshikonin

Cat.No: T3S2344

Synonym: β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin

Target: ERK, HIF/HIF Prolyl-Hydroxylase

Cat.No: T75451

Cat.No: TN4960

Target: Others

Cat.No: TN3740

Target: PAFR

Cat.No: TN3429

Target: Others

Cat.No: TN4340

Target: PARP

Hydroxytanshinone IIA

Cat.No: TN4239

Target: Others

Cat.No: TN5264

Target: TNF, NOS, ROS, COX, Antifection

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