296
32
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12030 |
MG 1
|
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
MG 1是一种有效的 α1肾上腺素能受体拮抗剂。 | |||
T6583 |
MG-101
ALLN,Ac-LLnL-CHO,Calpain inhibitor I,Calpain inhibitor-1,MG101,钙蛋白酶抑制剂I |
Cysteine Protease; Proteasome | Proteases/Proteasome; Ubiquitination |
MG-101 (Calpain inhibitor I) 是一种有效的半胱氨酸蛋白酶抑制剂,能够抑制钙蛋白酶I (Ki:190 pM),钙蛋白酶II (Ki:220 pM),组织蛋白酶B (Ki:150 pM)和组织蛋白酶L (Ki:500 pM)。 | |||
T12628 |
(R)-MG-132
(S,R,S)-(-)-MG-132,N-[(苯基甲氧基)羰基]-L-亮氨酰-N-[(1S)-1-甲酰基-3-甲基丁基]-D-亮氨酰胺,Z-Leu-D-leu-leu-al |
Proteasome | Proteases/Proteasome; Ubiquitination |
(R)-MG-132 (Z-Leu-D-leu-leu-al) 是一种 MG-132 的对映异构体,是一种蛋白酶体 (proteasome) 抑制剂,细胞毒性比 MG-132 弱,是一种比 MG-132 更有效的proteasome 抑制剂。 | |||
T4349 |
Sitravatinib
MG516,MGCD516 |
Discoidin Domain Receptor (DDR); VEGFR; FLT; Trk receptor; TAM Receptor; c-Kit; Ephrin Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。 | |||
T18391 |
N-Boc-4-pentyne-1-amine
|
Others; PROTAC Linker | Others; PROTAC |
N-Boc-4-pentyne-1-amine 是一种基于烷基链的PROTAC连结剂,用于PROTAC MG-277[1]的合成。 | |||
T35033L |
(S)-Vamicamide
(S)-Vamicamide (Iso-132373-81-0) |
AChE | Neuroscience |
(S)-Vamicamide 是一种新型抗抗胆碱能化合物。Vamicamide 在 32 mg/kg 或更高 (p.o.) 时增加小鼠的自发运动活动,并在 100 mg/kg 时抑制小鼠强直性惊厥。 | |||
T21617 |
MG-115
Z-LL-Nva-CHO |
Proteasome | Proteases/Proteasome; Ubiquitination |
MG-115 (Z-LL-Nva-CHO) 是一种有效且可逆的蛋白酶体抑制剂,对20S 和26S 蛋白酶体的 Ki 值分别为 21 nM 和 35 nM。MG-115 特异性抑制蛋白酶体的胰凝乳蛋白酶样活性,诱导 p53 依赖性细胞凋亡。 | |||
T15237 |
Eperezolid
PNU-100592 |
Antibacterial; Antibiotic | Microbiology/Virology |
Eperezolid (PNU-100592) 是一种在体外表现出良好抑制活性的恶唑烷酮类抗生素。 | |||
T1569 |
Tigecycline
替加环素,GAR-936 |
ribosome; Antibacterial; Antibiotic; Autophagy | Autophagy; Microbiology/Virology |
Tigecycline (GAR-936) 是甘氨酰环素抗生素,对 Acinetobacter baumannii(A. baumannii) 的 MIC50和 MIC90分别为 1 和 2 mg/L。它对 E. coli(MG1655 菌株) 的平均抑制浓度 (MIC) 约 125 ng/ mL。 | |||
T4039 |
BIBB 515
|
Others | Others |
BIBB 515 是口服具有活力的 2,3-氧化角鲨烯环化酶选择性抑制剂,在大鼠和小鼠中的 ED50值分别为 0.2-0.5 mg/kg 和 0.36-33.3 mg/kg (1-5 小时)。它主要利用抑制低密度脂蛋白的产生,从而发挥降脂作用。 | |||
T36569 |
KR-32568
|
Sodium Channel | Membrane transporter/Ion channel |
KR-32568是一种钠/氢交换器1(NHE-1)抑制剂(IC50:230 nM)。KR-32568具有强大的心脏保护作用。当使用浓度为10μM 时,它能在离体的缺血大鼠心脏模型中恢复心脏收缩功能。KR-32568(0.3mg/kg)在缺血和再灌注损伤的大鼠模型中减少了心肌梗死的大小。 | |||
T67956 |
Litoxetine
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
Litoxetine 是一种选择性的5-HT 摄取抑制剂,是具有5-HT3受体拮抗剂。Litoxetine 可作为一种抗抑郁剂,在雪貂身上显示出止吐特性。Litoxetine (1和10毫克/公斤静脉注射)剂量依赖性地减少了反胃和呕吐的次数,延迟了呕吐的发生。Litoxetine 对大脑5HT3受体有亲和力(Ki = 85 nM)。 | |||
T22697 |
CS 2100
1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid |
S1P Receptor | GPCR/G Protein |
CS 2100 (1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid) 是口服有活性 S1P3-sparingS1P1选择性激动剂,对人 S1P1的EC50值为 4.0 nM,对 HvGR 的ID50值为 0.407 mg/kg。它在大鼠体内具有免疫抑制作用。 | |||
T4436 |
RO1138452
CAY10441 |
Others; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Others |
RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂,pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活,以剂量依赖性方式阻断环 AMP 积累,具有镇痛活性。 | |||
T4306 |
CCG-203971
CCG203971 |
Rho; Ras | Cell Cycle/Checkpoint; GPCR/G Protein; MAPK |
CCG-203971 是一种Rho/MRTF/SRF 通路抑制剂,具有潜在的抗转移作用。它有效靶向 RhoA/C 激活的 SRE 荧光素酶,IC50为 6.4 μM。它抑制 PC-3 细胞迁移,IC50为 4.2 μM。 | |||
T38192 |
Unifiram
|
Others | Others |
Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。 | |||
T35689 |
MTP 131 acetate
|
Others | Others |
MTP 131 acetate 是一种小的线粒体靶向四肽。 | |||
T38050 |
CP-609754
|
Transferase | Metabolism |
CP-609754 是高效的、可逆的法尼基转移酶抑制剂,对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。 | |||
T36520 |
COR659
|
Cannabinoid Receptor; GABA Receptor | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。 | |||
T38294 |
4-Deoxypyridoxine hydrochloride
|
S1P Receptor | GPCR/G Protein |
4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解,与 S1P 一样,减少化学诱导的胰岛素瘤细胞系的细胞凋亡。 | |||
T36674 |
DMU-212
|
Apoptosis; ERK | Apoptosis; MAPK |
DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物,表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。 | |||
T36949 |
Niaprazine
|
5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Niaprazine 是有效的组胺 H1 受体拮抗剂,具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。 | |||
T36968 |
ARN-21934
|
Topoisomerase | DNA Damage/DNA Repair |
ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂,具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM,ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。 | |||
T63474 |
RyRs activator 1
|
||
RyRs activator 1 是兰尼碱受体 (RyRs) 的有效激活剂。RyRs activator 1 在 0.5 mg/L 时,杀幼虫活性为100%,在 0.01 mg/L 时,杀幼虫活性为90%。 | |||
T28391 |
PF-9404C
PF9404C |
||
PF-9404C is the S-S diesteroisomer of a beta adrenergic receptors blocker with vasodilatory properties. PF9404C increased the formation of cyclic GMP from 3 pmol mg−1 protein in basal conditions, to 53 pmol mg−1 protein in 10 μM in rat aorta smooth muscle | |||
T38272 |
Thiacloprid
|
AChR; Parasite | Microbiology/Virology; Neuroscience |
Thiacloprid 属于氯烟碱类杀虫剂,主要用于防治蔬菜和果园中的蚜虫。它会破坏 DNA 的稳定性,通过疏水或氢相互作用,结合到小沟槽中,改变 DNA 的结构和稳定性。 | |||
T28245 |
ONO-0300302
ONO 0300302 |
||
ONO-0300302 is a slow tight binding LPA1 antagonist (IC50: 0.16 nM) used to treat Benign Prostatic Hyperplasia. ONO-0300302 inhibits significantly an LPA-induced increase of intraurethral pressure (IUP) in rat (3 mg/kg, p.o.) and dog (1 mg/kg, p.o.) over | |||
T21968 |
MG-262
|
||
MG-262 是一种可逆的蛋白酶体抑制剂,具有多种生物活性。 | |||
T60949 | Complex III-IN-2 | ||
Complex III-IN-2 (Compd 4d-2) 是complex III 的抑制剂,具有抗真菌活性,其对植物病菌立枯病菌和核盘菌的EC50值分别为29.31 mg/L 和 29.98 mg/L。 | |||
T37657 | Mitochondrial respiration-IN-1 hydrobromide | ||
Mitochondrial respiration-IN-1 hydrobromide (compound 49) is a potent mitochondrial inhibitor (IC50=8.8 mg/mL). Mitochondrial respiration-IN-1 hydrobromide significantly reduces mitochondrial respiration in platelets[1]. | |||
T70344 |
BJ-2302
|
||
BJ-2302 is a SRC inhibitor. BJ-2302 effectively suppressed MDA-MB-231 cell invasion (Matrigel invasion assay) and metastasis (chorioallantoic membrane assay xenografted with MDA-MB-231-luc2-tdTomato cancer cells). Additionally, BJ-2302 (1 mg/kg) strongly suppressed TNBC cell proliferation in vitro and tumor growth in a xenograft mouse tumor model. The anti-metastatic and anti-tumor effects of BJ-2302 were superior to those of Z-FL-COCHO (1 mg/kg) or batimastat (30 mg/kg), a pan-MMP inhibitor. | |||
T81184 |
Sec61-IN-4
|
||
Sec61-IN-4(Compound 16b)作为Sec61抑制剂,其IC50值在U87-MG细胞中为0.04 nM。 | |||
T36599 |
4-Epianhydrotetracycline hydrochloride
|
||
Epianhydrotetracycline (EATC) is a degradation product of the antibiotic tetracycline .1 EATC is active against Pseudomonas, Agrobacterium, Moraxella, Bacillus, and E. coli (MIC50s = 0.75-16 mg/L). | |||
T37286 |
1-Undecanoyl-rac-glycerol
|
||
1-Undecanoyl-rac-glycerol is a monoacylglycerol that contains undecanoic acid at the sn-1 position. It completely inhibits the growth of the bacteria B. cereus, B. subtilis, M. luteus, E. faecalis, and S. aureus when used at concentrations ranging from 250 to 1,500 mg/L.1 1-Undecanoyl-rac-glycerol (0.1 and 0.3 mg/ml) also has antifungal activity against K. marxianus, S. cerevisiae, and C. maltosa.2 | |||
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 | |||
T61009 | Complex III-IN-1 | ||
Complex III-IN-1 (Compd 4c-2) 是 complex III 的抑制剂,具有抗真菌活性。Complex III-IN-1 对核盘菌的EC50值为 18.53 mg/L。 | |||
T82356 |
GABA-IN-1
|
||
GABA-IN-1 (Compound 6)为GABA抑制剂,具备显著的杀幼虫效能与杀虫功能,在浓度为50 mg/L时,致死率达93%。 | |||
T26610 |
AM-6761
AM 6761,AM6761 |
||
AM-6761 is a potent inhibitor of the MDM2-p53 interaction. In the SJSA-1 osteosarcoma xenograft model, AM-6761 shows excellent antitumor activity with an ED50 of 11 mg/kg. | |||
T83067 |
Antifungal agent 81
|
||
Antifungalagent 81(G22) 对马利弧菌显示出显著的体外抑制活性,其IC50为0.48 mg/L。在体内,以40 mg/L的剂量,Antifungalagent 81同样展现出对马里弧菌的良好保护效果。 | |||
T7720 |
CGP 37849
CGP-37849,CGP37849 |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
CGP 37849 是一种竞争性口服活性 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂((Ki = 35 nM)),具有有效性。CGP 37849 是啮齿动物的抗惊厥药,也具有抗抑郁和抗焦虑的特性。 | |||
T79399 | E2730 | GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
E2730是一种针对γ-氨基丁酸(GABA)转运蛋白1(GAT1)的非竞争性选择性抑制剂,它能口服有效且有抗癫痫的作用。这种化合物能够随着环境中GABA水平的增加而增强其抑制GAT1的活性,从而有选择性地抑制GABA的回收。在实验模型中,E2730 (剂量范围为5-50 mg/kg; 经口给药) 在大鼠杏仁核点燃模型和小鼠的多种癫痫模型中,包括角膜点燃 (5-50 mg/kg)、耐药的6Hz-44mA精神运动癫痫 (5-50 mg/kg)、脆性X综合征 (2.5-300 mg/kg) 及Dravet综合征模型 (10 mg/kg, 20 mg/kg),展现了显著的体内活性。 | |||
T78804 |
PI3Kα-IN-12
|
PI3K | PI3K/Akt/mTOR signaling |
PI3Kα-IN-12(化合物13),作为一种高度选择性的PI3Kα抑制剂,展现出了1.2 nM的IC50值。在HCT-116和U87-MG细胞线上的抑制作用,IC50s分别为0.83 μM和1.25 μM。通过腹腔注射(IP)给予40 mg/kg的PI3Kα-IN-12,能够有效引起接受U87-MG细胞系异种移植的小鼠模型中的肿瘤退缩。 | |||
T79682 |
qsl-304
|
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
QSL-304为一种DNA旋转酶B抑制剂,并具有抗菌作用,其对金黄色葡萄球菌sa-P2003的IC50值为31.23 mg/mL。 | |||
T81237 |
RyRs activator 4
|
||
RyRs activator 4为一款昆虫兰尼碱受体激活剂,对粘虫幼虫显示出显著的杀灭活性,其半致死浓度(LC50)为1.32 mg/L。 | |||
T61255 |
SDH-IN-1
|
||
SDH-IN-1 (compound 4i) is a potent succinate dehydrogenase (SDH) inhibitor, exhibiting an IC 50 value of 4.53 μM. This compound displays strong antifungal properties, particularly against S. sclerotiorum, with an EC 50 value of 0.14 mg/L [1]. | |||
T82834 |
Bombinin-BO1
|
||
Bombinin-BO1是一种蟾蜍皮肤分泌物中的抗菌肽,它对大肠杆菌(Escherichia coli)、金黄色葡萄球菌(Staphylococcus aureus)和白色念珠菌(Candida albicans)显示出抗生活性,其最小抑菌浓度(MIC)值分别为64 mg/L, 64 mg/L和128 mg/L。 | |||
T75279 | Tigecycline tetramesylate | ||
Tigecycline tetramesylate (GAR-936 tetramesylate)为一款广谱甘氨酰环素类抗生素,对E. coli (MG1655菌株)展现出约125 ng/mL的平均抑制浓度(MIC)。针对Acinetobacter baumannii (A. baumannii)的MIC50与MIC90分别达到1 mg/L与2 mg/L。 | |||
T79544 |
SDH-IN-6
|
||
SDH-IN-6 (compound 6i)是琥珀酸脱氢酶(SDH)的高效抑制剂,并显示出对Valsa mali的抗真菌活性,其EC50为1.77 mg/L。 | |||
T82355 |
GABA-IN-2
|
||
GABA-IN-2 (Compound 5) 为GABA抑制剂,展现出杀幼虫效果和显著的杀虫能力,在浓度50 mg/L下的死亡率达到87%。 | |||
T82835 |
Bombinin H-BO1
|
||
Bombinin H-BO1 是源自蟾蜍皮肤分泌物的抗菌肽,对白色念珠菌有效,其MIC值达256 mg/L。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S2252 |
Sweroside
|
Others | Others |
Sweroside 是分离自Lonicera japonica 中,具有细胞保护、抗骨质疏松和保护肝脏活性。 | |||
T6S0033 |
Crotonoside
巴豆苷;异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE |
Others; FLT; HDAC | Angiogenesis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Others; Tyrosine Kinase/Adaptors |
Crotonoside (Isoguanosine) 是从中草药巴豆中分离出来的一种天然产物。 它抑制 FLT3 和 HDAC3/6,有治疗急性髓性白血病 (AML)的研究潜力。 | |||
T2S0493 |
Isoeugenol
4-Propenylguaiacol,2-Methoxy-4-propenylphenol,异丁香酚,异丁香酚;4-丙烯基-2-甲氧基苯酚、对丙烯基邻甲氧基本酚、异丁子香酚 |
Antibacterial | Microbiology/Virology |
Isoeugenol (4-Propenylguaiacol) 是肉豆蔻,丁香和肉桂的精油成分,具有抗菌活性。它抑制Escherichia coli 和Listeria innocua,MIC 值分别为 0.6 mg/mL 和 1 mg/mL。 | |||
T5269 |
N-Acetylornithine
Acetyl-ornithine,N-Acetyl-L-ornithine,N-乙酰鸟氨酸 |
Others; Endogenous Metabolite | Metabolism; Others |
N-Acetylornithine (N-Acetyl-L-ornithine) 是一种人内源性代谢物,是 L-谷氨酸到 L-精氨酸的酶促合成中的中间体。 | |||
T5S1989 |
Apiin
Apioside,芹菜苷 |
Others | Others |
Apiin (Apioside) 是Apium graveolens 叶片的一种主要成分,具有抗炎作用。它在体外抑制亚硝酸盐产生的IC50值为0.08 mg/mL,在 LPS 激活的 J774.A1 细胞中抑制 iNOS 的表达的IC50值为0.049 mg/ mL。 | |||
T3868 |
Agnuside
牡荆油,穗花牡荆苷,chasteberry oil |
COX; Prostaglandin Receptor; P-gp | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience |
Agnuside (chasteberry oil) 是从黄荆中分离得到的一种天然产物,可下调炎性介质PGE2和LTB4,减少细胞因子的表达,具有抗关节炎活性。 | |||
T6S1141 |
Ganoderic acid A
灵芝酸 A,灵芝酸A |
Apoptosis; NF-κB; Endogenous Metabolite; Autophagy | Apoptosis; Autophagy; Metabolism; NF-κB |
Ganoderic acid A 能够抑制 JAK-STAT3信号通路,也能抑制细胞增殖,存活率和 ROS。 它对人骨肉瘤 HOS 和MG-63细胞具有增殖抑制、凋亡和侵袭抑制作用。 | |||
TCS1704 |
Artemitin
艾黄素,Artemetin,Artemisetin,Erianthin |
Antioxidant | oxidation-reduction |
Artemitin (Erianthin) 是一种存在于翼齿六棱菊中的天然黄酮,具有抗氧化、抗炎、抗病毒活性。 | |||
T4904 |
1-Methylguanidine hydrochloride
|
Others; Endogenous Metabolite | Metabolism; Others |
1-Methylguanidine hydrochloride 是内源性代谢产物的一种。 | |||
T4439 |
sn-Glycero-3-phosphocholine
Choline Alfoscerate,甘磷酸胆碱,Glycerophosphocholine,Glycerophosphorylcholine,Alpha-GPC,Choline glycerophosphate,L-α-GPC |
Endogenous Metabolite; AChE | Metabolism; Neuroscience |
sn-Glycero-3-phosphocholine (Choline glycerophosphate) 是脑磷脂生物合成的前体,能够提高胆碱在神经组织中的生物利用度。它对认知功能有显著影响,同时具有良好的耐受性和安全性,因此能够用于阿尔茨海默病和痴呆症的研究。 | |||
T2776 |
Tribuloside
Tiliroside,刺蒺藜皂甙,蒺藜皂甙 |
Others; Antibacterial | Microbiology/Virology; Others |
Tribuloside (Tiliroside) A 是一种可从 Tribulus terrestris L 中分离得到的黄酮,可抑制非致病性分枝杆菌,MIC 值 为5.0 mg/mL。 | |||
TWS2045 |
Bruceine D
鸦胆子素D,鸦胆子苦素D |
Apoptosis; Antiviral; Gamma-secretase; Parasite | Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells |
Bruceine D 是Notch 抑制剂,有抗癌活性,诱导几种人癌细胞调亡。它是一种有效的植物性昆虫拒食剂,有显著的系统特性和抑制害虫生长的作用。它具有较强的驱虫活性,抑制D. intermedius 的 EC50值为 0.57 mg/L。 | |||
T72742 |
(-)-Pinocembrin
(-)-乔松素 |
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(-)-Pinocembrin 对 H37Ra 结核分枝杆菌展示了抗菌活性,无论是休眠还是活跃期,其 IC50 值分别为1.11 mg/mL 和 1.21 mg/mL。作为一种抗增殖剂,(-)-Pinocembrin 对于 THP-1、A549、Panc-1、HeLa 和 MCF7 细胞系,IC50 值范围为 1.88 至 11.00 mg/mL。 | |||
T83254 |
7,4'-Dihydroxyhomoisoflavane
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7,4'-Dihydroxyhomoisoflavane 是一种具有抗氧化能力的天然化合物,能有效清除 ABTS 自由基,其半抑制浓度 (IC50) 为 0.22 mg/mL。 | |||
T79958 |
Isocrenatoside
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Angiotensin-converting Enzyme (ACE) | Metabolism |
Isocrenatoside (compound 6)为环状八肽,具有ACE抑制活性。该化合物可通过乙醇提取Microtoena prainiana茎部分离纯化。研究显示,1 mg/mL浓度下,Isocrenatoside的ACE抑制效率高达99.3%。 | |||
T75701 | 8,3′,4′-Trihydroxyflavone-7-O-β-D-glucopyranoside | ||
8,3′,4′-Trihydroxyflavone-7-O-β-D-glucopyranoside (Compound 3) 是一种可以从Bidens bipinnata 分离得到的天然产物。8,3′,4′-Trihydroxyflavone-7-O-β-D-glucopyranoside 在 0.556 mg/mL 时对α-amylase 有 22% 的抑制作用。 | |||
T37444 |
Aranorosin
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Aranorosin is a fungal metabolite originally isolated from P. roseus. It has antimicrobial activity against B. subtilis, A. niger, and C. albicans when used at a concentration of 1 mg/ml. Aranorosin also reduces viability in apoptosis-resistant HeLa/Bcl-2 cells. | |||
T83920 |
4-Trehalosamine
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4-Trehalosamine是一种在Streptomyces中发现的微生物代谢产物,具有抗生素活性。在杯碟法测试中,当浓度为0.5、1和2 mg/ml时,对E. coli、K. pneumoniae和B. subtilis展现出活性。 | |||
T35532 |
Galegine hydrochloride
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Galegine hydrochloride, a guanidine derivative derived from G. officinalis, plays a role in inducing weight loss in mice and has contributed to the development of biguanides, including metformin and phenformin. This compound stimulates AMPK activation in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cell lines. Additionally, galegine hydrochloride exhibits antibacterial properties, particularly demonstrating a minimum inhibitory concentration of 4 mg/L against Staph... | |||
T83903 |
Polymyxin B2 sulfate
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Polymyxin B2是一种抗生素,并且是从B. polymyxa分离出的阳离子脂肽抗生素polymyxin B的主要成分。该化合物对P. aeruginosa、A. baumannii、K. pneumoniae和E. cloacae菌株具有活性(MICs分别为1-2、0.5-1、0.25-0.5和0.25-1 µg/ml)。在体内实验中,以4 mg/kg剂量的Polymyxin B2能显著降低P. aeruginosa血液感染小鼠模型中的血液集落形成单位(CFUs)数量。 | |||
T35624 |
Ajoene
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Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces... | |||
T66078 | Cardamonin | ||
Cardamonin, a chalcone extracted from cardamom spice with anti-inflammatory and anti-tumor activities. Cardamonin decreased viability of NPC(Nasopharyngeal carcinoma ) cells in a concentration-dependent manner. The IC50 values were 16.22 μM(CNE-1), 14.34 μM (CNE-2), 16.50 μM (HONE-1), and 68.12 μM (SUNE-1). Moreover, the expression level of the proapoptotic effector protein Bax and Bid was also markedly increased after treatment with cardamonin(15μM) in CNE-2 cells.In vivo, cardamonin (25 mg/kg ... | |||
T36179 |
Aspulvinone O
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Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) redu... | |||
T83915 |
Norbixin hydrate
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Norbixin是一种在B. orellana中发现的类胡萝卜素,具有多样的生物活性。在无细胞测试中,它与过氧化物酶体增殖物激活受体γ (PPARγ)结合(Ki = 1.15 µM)。在心脑血管代谢综合征大鼠模型中,Norbixin (47.7 mg/kg) 能够减轻高血糖、高胰岛素血症和胰岛素抗性,降低血清脂质水平及心脏中硫代巴比妥酸反应性物质(TBARS)和谷胱甘肽(GSH)的水平。在胆固醇诱导的动脉粥样硬化兔模型中,它降低氧化型LDL和主动脉蛋白氧化水平,并减少动脉粥样硬化面积。Norbixin(每天0.1和1 mg/kg)减少汞诱导的大鼠肝细胞和白细胞DNA损伤。此外,它还能预防与年龄相关的黄斑变性(AMD)Abca4-/- Rdh8-/-小鼠模型中的光感受器退化。 | |||
T35752 |
Xanthoquinodin A1
Xanthoquinodin A1 |
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Xanthoquinodin A1 is a fungal metabolite that has been found inHumicolaand has diverse biological activities.1,2It inhibitsE. tenellaschizont formation in BHK-21 cells with a minimum effective concentration (MEC) value of 0.02 μg/ml.1Xanthoquinodin A1 is active againstB. subtilis,M. luteus,S. aureus,A. laidlawii, andB. fragilisin a disc assay when used at a concentration of 1 mg/ml. It is also active againstB. cereus(MIC = 0.44 μM).2Xanthoquinodin A1 is cytotoxic to KB, MCF-7, and NCI H187 cance... | |||
T35750 |
Trypacidin
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Trypacidin is a fungal metabolite originally isolated fromA. fumigatus.1It is active againstB. subtilisandM. bovis(MICs = 12.5 and 1.25 μg/ml, respectively), as well asT. cruziandT. gondii(MICs = 5-10 and 10-20 μg/ml, respectively).1,2It reduces viability and induces lysis of A549 human lung cancer cells (IC50s = 7.4 μM for both).3Trypacidin increases survival in a mouse model ofT. gondiiinfection when administered in six doses of 12.5 mg/kg each.1 1.Balan, J., Ebringer, L., Nemec, P., et al.Ant... | |||
T37609 |
(rel)-Asperparaline A
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Aspergillimide is a fungal metabolite originally isolated from A. japonicus.1 It reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons (IC50s = 20.2 and 39.6 nM, respectively) but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.2 Dietary administration of aspergillimide A (10 μg/g of diet) induces paralysis in silkworm fourth instar larvae.1 Aspergillimide A (10 and 20 mg/kg) reduces... | |||
T36227 |
Beauveriolide III
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Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg/kg) reduces the size of aortic ... | |||
T35751 |
Violacein
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Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active aga... | |||
T35779 |
Oosporein
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Oosporein is a mycotoxin that has been found inBeauveriaand has diverse biological activities.1,2It is cytotoxic to Sf9 and Sf21 insect cells with 50% cytotoxic concentration (CC50) values of 4.23 and 10.43 μM, respectively.3Oosporin induces lethality in day-old cockerels (LD50= 6.12 mg/kg).4It inhibits Na+/K+-, Ca2+-, and Mg2+-ATPase activities by 27, 52, and 100%, respectively, in equine erythrocyte ghosts when used at a concentration of 200 μg/ml.2Oosporein inhibits herpes simplex 1 (HSV-1), ... | |||
T36448 |
(E)-Ajoene
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(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanoth... | |||
T36954 |
Nemorosone
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Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem... |