101
21
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11738 |
K-Ras G12C-IN-4
|
Ras | GPCR/G Protein; MAPK |
K-Ras G12C-IN-4 是一种 KRAS G12C 共价抑制剂。 | |||
T25094 |
Antibiotic K 4
I5B1,I5 B1,K-4,K4,I5-B1 |
||
Antibiotic K 4 is an inhibitor of angiotensin I converting enzyme produced by Actinomadura spiculosospora. | |||
T18057 |
K-Ras ligand-Linker Conjugate 4
|
Others | Others |
K-Ras ligand-Linker Conjugate 4 is a chemical compound that combines a ligand for K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The compound has the potential to be used in the synthesis of PROTAC K-Ras Degrader-1, a powerful degrader of K-Ras that has been shown to exhibit a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T11942 |
MAP4K4-IN-3
Compound 17 |
MAPK | MAPK |
MAP4K4-IN-3 (Compound 17) 是 MAP4K4选择性抑制剂,在激酶实验中 IC50为 14.9 nM,在细胞实验中 IC50为 470 nM。具有抗糖尿病作用。 | |||
T13631L |
c(phg-isoDGR- (NMe)k) TFA (1844830-65-4 free base)
c(phg-isoDGR-(NMe)k) TFA |
Others | Others |
c(phg-isoDGR-(NMe)k) TFA is a potent and selective α5β1-integrin ligand (IC50: 2.9 nM). | |||
T39452 |
PIP4K-IN-a131
PIP4K-IN-a131 |
||
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC 50 s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways. | |||
T35527 |
PI3Kα-IN-4
PI3Kα-IN-4 |
||
PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t... | |||
T35488 |
(S)-PI3Kα-IN-4
(S)-PI3Kα-IN-4 |
||
(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitor... | |||
T80321 |
The K4 peptide
|
||
K4 peptide 是一种抗菌肽,对革兰氏阳性细菌和革兰氏阴性细菌均显示出显著活性,能够有效作用于包括金黄色葡萄球菌和弧菌属海洋细菌在内的多种人类致病菌。 | |||
T79794 |
TNIK&MAP4K4-IN-1
|
||
TNIK&MAP4K4-IN-1(化合物A-39)作为TNIK和MAP4K4/HGK的双效抑制剂,在LX-2人肝星状细胞中,其IC50为1.29 nM和<10 nM。该化合物适用于癌症和纤维化治疗。 | |||
T74660 |
M4K2234
|
||
M4K2234 (compound 26b) 是 ALK2的抑制剂。M4K2234 抑制 ALK2和 ALK5的 IC50值分别为 5 和 2144 nM。M4K2234 可用作 ALK1和 ALK2蛋白激酶的化学探针。M4K2234 可用于癌症的研究。 | |||
T70148 |
CDK8-IN-4k
|
||
CDK8-IN-4k is a potent and highly selective CDK8 inhibitor, with no apparent potential for time-dependent CYP3A4 inhibition. | |||
T62165 |
PI3Kγ inhibitor 4
|
||
PI3Kγ inhibitor 4 是一种选择性的、有效的、口服具有活力的 PI3Kγ 抑制剂 (IC50: 40 nM)。PI3Kγ inhibitor 4 对 PI3Kγ 的选择性是 α 亚型的~7 倍、是 β 亚型的 43 倍、是 δ 亚型的 18 倍。PI3Kγ inhibitor 4 能够用于研究气道炎症。 | |||
T61971 |
CHMFL-PI4K-127
|
||
CHMFL-PI4K-127 (compound 15g) 是具有口服活性、高选择性的PfPI4K(恶性疟原虫 PI4K 激酶)抑制剂(IC50= 0.9 nM)。CHMFL-PI4K-127 对 3D7 恶性疟原虫表现出较强的抑制活性(EC50= 25.1 nM)。CHMFL-PI4K-127 具有抗疟疾作用。 | |||
T83312 |
4N1K peptide
|
||
4N1K peptide 是具有抗癌活性的生物活性肽,源于血小板反应蛋白中的 4N1K 肽序列(KRFYVVMWKK),能够对抗多种癌症。 | |||
T63770 |
PI3K/mTOR Inhibitor-4
|
||
PI3K/mTOR Inhibitor-4 是一种口服具有活力的泛 I 类 PI3K/mTOR 抑制剂。PI3K/mTOR Inhibitor-4 具有酶抑制作用,能够作用于 PI3Kα (IC50: 0.63 nM)、PI3Kγ (IC50: 22 nM)、PI3Kδ (IC50: 9.2 nM) 和 mTOR (IC50: 13.85 nM)。PI3K/mTOR Inhibitor-4 能够用于研究癌症。 | |||
T81465 |
PI5P4K-β-IN-1
|
||
PI5P4K-β-IN-1(compound vs1)是一款针对PI5P4K-β具有高效抑制活性的化合物,其IC50值为0.80 μM。 | |||
T78178 |
PI5P4Kα-IN-1
|
Others | Others |
PI5P4Kα-IN-1(化合物13)是一种针对PI5P4Kα和PI5P4Kβ具有选择性抑制作用的化合物(IC50分别为2 μM和9.4 μM)。它适用于癌症、代谢和免疫紊乱相关研究。 | |||
T81464 |
PI5P4K-β-IN-2
|
||
PI5P4K-β-IN-2 (compound d5)为一种PI5P4K-β抑制剂,IC50值为0.35 μM,展现出抗癌活性。 | |||
T8936 |
Proteinase K
proteinase K for tritirachium album,Protease K,蛋白酶 K |
Others | Others |
Proteinase K (proteinase K for tritirachium album) 是一种非特异性丝氨酸蛋白酶,可用于蛋白消化。它在有 SDS 或尿素存在的情况下,在很大 pH 值 (4-12)、盐浓度和温度单位内均有活性。 | |||
T71708 |
Minamestane
|
Aromatase | Endocrinology/Hormones |
Minamestane 是一种新型不可逆芳香化酶抑制剂。Minamestane 引起人胎盘芳香化酶的时间依赖性抑制,半衰期为4分钟,K 为59nM。Minamestane 具有抗肿瘤活性。 | |||
T67947 |
WDR5-0102
|
Histone Methyltransferase | Chromatin/Epigenetic |
WDR5-0102为针对WDR5-MLL1的抑制剂(Kdis=7 μM, Kd=4 μM)。该化合物有效抑制MLL1活性,而对人类H3K4甲基转移酶SETD7及其他六种HMT(G9a、EHMT1、SUV39H2、SETD8、PRMT3、PRMT5)不表现出抑制作用。 | |||
T26086L |
1-((3R,4S)-3-hydroxy-2,2-dimethyl-6-(phenylsulfonyl)chroman-4-yl)pyrrolidin-2-one
|
Others | Others |
1-((3R,4S)-3-hydroxy-2,2-dimethyl-6-(phenylsulfonyl)chroman-4-yl)pyrrolidin-2-one 是 Rilmakalim 的异构体,Rilmakalim 是一种钾通道打开剂 (PCO),可以激活心脏或其它组织中 ATP-敏感 K+ 通道 | |||
T60248 |
4-Aminobenzamidine dihydrochloride
p-Aminobenzamidine dihydrochloride |
Serine Protease | Proteases/Proteasome |
4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) 是一种强胰蛋白酶 (trypsin)抑制剂,也是一种相对较弱的尿激酶型纤溶酶原激活剂 (uPA) 抑制剂 (Ki=82 μM)。4-Aminobenzamidine 可抑制 SCID 小鼠体内前列腺肿瘤的生长。 | |||
T1651 |
Rabeprazole sodium
Dexrabeprazole Sodium,LY307640 sodium,Habeprazole Sodium,雷贝拉唑钠,Rebeprazole sodium,Aciphex Sodium |
Apoptosis; Proton pump | Apoptosis; Membrane transporter/Ion channel |
Rabeprazole sodium (Habeprazole Sodium) 是一种质子泵抑制剂,不可逆地抑制胃 H+/K+-ATPase,可研究胃溃疡和胃食管反流。它诱导细胞凋亡,也抑制尿苷核苷核糖水解酶 ,IC50为 0.3 μM。 | |||
T38941 |
FPI-1523 sodium
|
Endogenous Metabolite; Antibacterial | Metabolism; Microbiology/Virology |
FPI-1523 sodium 是阿维巴坦的衍生物,是一种强效的 β-内酰胺酶抑制剂,对 CTX-M-15 和 OXA-48 的 K d s 分别为 4 nM 和 34 nM。FPI-1523 sodium 对 PBP2 有抑制作用,其 IC 50 为 3.2 μM。FPI-1523 sodium具有相当高的抗菌活性。 | |||
T17243 |
VU0463271
N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide |
Potassium Channel | Membrane transporter/Ion channel |
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) 是一种有效的、特异性的 KCC2 拮抗剂,其 IC50 为 61 nM,特异性是密切相关的 Na-K-2Cl 协同转运蛋白 1 (NKCC1) 的 100 倍以上,在更大的 GPCR、离子通道和转运蛋白面板中没有活性。 | |||
T41275 |
PF-04753299
|
Others | Others |
PF-04753299 是一种有效的、选择性的LpxC 抑制剂。PF-04753299 对淋球菌分离株具有杀菌作用,对大肠杆菌、铜绿假单胞菌和肺炎菌株的抑制的MIC90值分别为 2 μg/ml、4 μg/ml 和 16 μg/ml。PF-04753299 用于革兰氏阴性菌感染的研究。 | |||
T4980 |
Betrixaban maleate
|
Factor Xa | Metabolism |
Betrixaban maleate 是一种非维生素 K 口服抗凝剂,其作用是由 Xa 因子的竞争性和可逆抑制作用驱动的。 | |||
T4341 |
Betrixaban
贝曲西班,PRT054021 |
Factor Xa | Metabolism |
Betrixaban (PRT054021) 是一种口服具有活力的选择性factor Xa(fXa) 抑制剂,IC50=1.5 nM。 | |||
T3148 |
MK-571 sodium
L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid |
Leukotriene Receptor; LTR | GPCR/G Protein; Immunology/Inflammation |
MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂,在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。 | |||
T1278 |
Astemizole
Laridal,Histaminos,Paralergin,阿司咪唑 |
Potassium Channel; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience |
Astemizole (Laridal) 是一种长效、非镇静抗组胺药,用于治疗季节性过敏性鼻炎、哮喘、过敏性结膜炎和慢性特发性荨麻疹。它是组胺 H1 受体的拮抗剂,IC50值为 4 nM,还阻断 hERG K+通道,IC50值为 0.9 nM,具有抗胆碱能和止痒作用。 | |||
T25809 |
MI-14
MI14 |
||
MI-14 is a potent and selective inhibitor of PI 4-K IIIß. | |||
T40738 |
CAY10580
CAY10580 |
||
CAY10580 is a potent and selective prostaglandin EP 4 receptor agonist ( K i =35 nM). | |||
TP2089 |
Agitoxin-2
Agitoxin 2 |
||
Potent Shaker K+ channel blocker (Ki = 0.64 nM). Also inhibits Kv1.3, Kv1.6 and Kv1.1 K+ channels (Ki values are 4, 37 and 44 pM respectively). | |||
T83944 |
IPG-4 AM
|
||
IPG-4 AM 是一种可渗透膜的荧光钾离子 (K+) 指示剂,具有与钾结合的特性 (Kd= 7 mM)。其激发和发射峰值 (λ) 分别为 525 和 545 nm。它对 K+ 比 Na+ 离子具有 100:1 的选择性。可用于实时检测细胞内 K+ 的变化,也用于监测体内外 K+ 的变化。 | |||
T61829 | Carbonic anhydrase inhibitor 4 | ||
Carbonic anhydrase inhibitor 4 is a photoprobe that inhibits the activity of carbonic anhydrase. It specifically targets human carbonic anhydrases, including hCA I-XIV, with K i values ranging from 640-1166 nM [1]. | |||
T61558 |
HBV-IN-21
|
||
HBV-IN-21 (Compound II-8b) is a potent inhibitor of HBV DNA replication, exhibiting an IC50 of 2.2 μM. It demonstrates a favorable binding affinity (K D = 60.0 μM) for the HBV 4 capsid protein, thereby enabling effective interaction [1]. | |||
T75749 |
Galantide TFA
|
||
Galantide TFA 是一种可逆的非特异性甘丙肽 galanin(GAL)受体拮抗剂。Galantide TFA 剂量依赖性显示出对 galanin 诱导的 K+电导的拮抗作用,IC50值为 4 nM。Galantide TFA 可用于神经疾病和激素代谢的研究。 | |||
T83719 |
Mca-AVLQSGFR-K(Dnp)-K-NH2 TFA
|
||
Mca-AVLQSGFR-K(Dnp)-K-NH2 是针对严重急性呼吸综合征冠状病毒(SARS-CoV)主蛋白酶(Mpro),也称为3C样蛋白酶(3CLpro)的荧光底物。SARS-CoV Mpro 切割后,会释放7-甲氧基香豆素-4-乙酰基(Mca),通过其荧光可以量化SARS-CoV Mpro 活性。Mca 的激发/发射波长最大值分别为328/420 nm。 | |||
T73372 |
GNE-2256
|
||
GNE-2256 (molecule 19) 是一种具有口服活性的IRAK4(白介素 1 受体关联激酶 4) 抑制剂 (IRAK4Ki=1.4 nM ; IL-6IC50=190 nM)。 | |||
T38646 |
GKT136901 hydrochloride
GKT136901 hydrochloride |
||
GKT136901 hydrochloride is a powerful, selective, and orally active inhibitor of NADPH oxidase (NOX1/4). It exhibits K i values of 160 nM and 165 nM against NOX1 and NOX4, respectively. Additionally, GKT136901 hydrochloride demonstrates selectivity and direct scavenging ability towards peroxynitrite. This compound finds utility in studying diabetic nephropathy, stroke, neurodegeneration, and possesses anti-inflammatory properties. | |||
T79451 | WES-1 | Carbonic Anhydrase | Metabolism |
WES-1(Compound 8g)是一种针对碳酸酐酶IX的抑制剂,其抑制常数(Ki)为55.9 μM。该化合物对包括白血病细胞系(K-562、MOLT-4)、非小细胞肺癌(NCI-H460)、结肠癌(HCT 116、HCT-15)以及黑色素瘤(LOX IMVI)在内的多种癌细胞表现出抗增殖效果。 | |||
T74980 | SPAA-52 | ||
SPAA-52 是一种具有口服活性的、竞争性的和可逆的低分子量蛋白酪氨酸磷酸酶 (LMW-PTP) 抑制剂 (IC50=4 nM,Ki=1.2 nM)。SPAA-52 可用于糖尿病的研究。 | |||
T83686 |
Mca-SEVNLDAEFR-K(Dnp)-RR-NH2 acetate
|
||
Mca-SEVNLDAEFR-K(Dnp)-RR-NH2是β-分泌酶(BACE)的荧光底物。当BACE切割该底物时,7-甲氧基香豆素-4-乙酰基(Mca)会被释放出来,其荧光可用于定量BACE活性。Mca的激发/发射最大值分别为328/420 nm。 | |||
TP2114 |
Tertiapin-Q
|
||
A high affinity blocker for inward-rectifier K+ channels, this compound is a stable derivative of the bee venom toxin tertiapin. Binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with high affinity (Ki values are 1.3 and 13.3 nM respectively) and | |||
T76596 |
PRL 3195
|
||
PRL 3195 是一种somatostatin receptor 拮抗剂,对人生长抑素受体 sst5、sst2、sst3、sst1和 sst4的Ki 分别为 6、17、66、1000 和 1000 nM。 | |||
T39790 |
LpxC-IN-5
|
||
LpxC-IN-5 is a potent, non-hydroxamate inhibitor of LpxC, which is an enzyme known as UDP-3-O-acyl-N-acetylglucosamine deacetylase. It exhibits an IC50 value of 20 nM. Furthermore, LpxC-IN-5 displays antibacterial activity against various strains including E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883, and P. aeruginosa 5567. The minimum inhibitory concentration (MIC) values for these strains are 16 μg/mL, 4 μg/mL, 64 μg/mL, and 4 μg/mL, respectively. | |||
T73724 | WDR5-IN-4 TFA | ||
WDR5-IN-4 TFA 是一种染色质相关 WD 重复结构域 5 蛋白 (WDR5) 的 WIN 位点抑制剂,Kd 值为 0.1 nM。WDR5-IN-4 TFA 能够从染色质中取代 WDR5,并降低相关基因的表达,引起翻译抑制和核仁应激。具有抗癌作用。 | |||
T26657 |
AR-H067637
|
||
AR-H067637 is a rapid-binding, reversible and potent (inhibition constant K(i) = 2-4 nM), competitive inhibitor of thrombin, as well as of thrombin bound to fibrin (clot-bound thrombin) or to thrombomodulin. The total amount of free thrombin generated in |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2570 |
Vitamin K4
维生素K4,维生素 K4,Kapilin,Menadiol Diacetate,acetomenaphthone |
Apoptosis; Endogenous Metabolite | Apoptosis; Metabolism |
Vitamin K4 (Menadiol Diacetate) 是一种维生素药物,用于治疗因缺乏 VK4 引起的凝血障碍。 | |||
T7106 |
Menaquinone-4
四烯甲萘醌,Vitamin K2,Menaquinone K4 |
Others; Endogenous Metabolite | Metabolism; Others |
Menaquinone-4 (Vitamin K2) 是维生素 K 的一种,用作止血剂,有潜力用于骨质疏松的研究。 | |||
TN1631 |
Eupalinolide K
[3AR-[3AR*,4R*(E),6E,9S*,10E,11AR*]]-4-羟基-2-甲基-2-丁烯酸 2,3,3A,4,5,8,9,11A-八氢-9-羟基-6,10-二甲基-3-亚甲基-2-氧代环癸五烯并[B]呋喃-4-基酯,野马追内酯 K,野马追内酯K |
STAT | JAK/STAT signaling; Stem Cells |
Eupalinolide K 是来自野马追的一种倍半萜内酯,是 STAT3抑制剂,可作为迈克尔反应受体。 | |||
TN1328 |
7-Amino-4-methylcoumarin-3-acetic acid
7-氨基-4-甲基-3-香豆素醋酸,7-Amino-4-methylcoumarin |
Others | Others |
7-Amino-4-methylcoumarin-3-acetic acid (7-Amino-4-methylcoumarin) 是荧光蛋白质标记剂,能够被紫外光(350 nm) 激活,可在蓝色区域 (440-460 nm) 发光。 | |||
TN2019 |
Orobol
3'-Hydroxygenistein,3’,4’,5,7-tetrahydroxy-isoflavon,3',4',5,7-四羟基异黄酮 |
BCL; Caspase; PI3K | Apoptosis; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Orobol (3’,4’,5,7-tetrahydroxy-isoflavon) 是酪氨酸特异性蛋白激酶和磷脂酰肌醇转换的抑制剂。Orobol 抑制 PI3K,对 PI3K α/β/γ/K/δ 的 IC50 为 3.46-5.27 μM。 Orobol 具有抗皮肤老化和抗肥胖的作用。 | |||
T4A2458 |
Resibufogenin
酯蟾毒配基,Bufogenin,Recibufogenin,酯蟾毒配基,蟾力苏 |
Others | Others |
Resibufogenin (Bufogenin) 是华蟾素的成分之一,表现出抑制氧化应激及肿瘤再生的活性。 | |||
TJP2872 |
Acevaltrate
Acevaltratum,乙酰缬草三酯,Acetoxyvaltrate |
ATPase; Others | Membrane transporter/Ion channel; Others |
Acevaltrate (Acevaltratum) 对人小细胞肺癌细胞系 GLC(4) 和人结肠直肠癌细胞系 COLO 320 具有高细胞毒性,IC50 值为 1-6 uM。它抑制大鼠肾和脑半球中 Na+/K+-ATP 酶活性,IC50分别为 22.8 和 42.3 μM。 | |||
TCS2170 |
2,5-Dihydroxyacetophenone
Quinacetophenone,2-Acetylhydroquinone,2-5-dihydroxyacetophenone,2 ',5'-二羟基苯乙酮,Acetylhydroquinone,2,5-二羟基苯乙酮,DHAP |
ERK; NF-κB; Tyrosinase | MAPK; NF-κB; Proteases/Proteasome |
2,5-Dihydroxyacetophenone (Quinacetophenone) 是从熟地黄中分离出的一种天然产物,通过阻断 ERK1/2和 NF-κB 信号通路,抑制活化巨噬细胞中炎症介质的产生。 | |||
TN4805 |
Platycoside K
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Others | Others |
Platycoside K 是一种天然产物,可用于生命科学领域的相关研究。其产品编号为 TN4805,CAS号为 899447-64-4。 | |||
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。 | |||
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。 | |||
T80001 |
Majoranaquinone
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Antibiotic | Microbiology/Virology |
Majoranaquinone对4种Staphylococcus菌株、1种Moraxella菌株和1种Enterococcus菌株显示出良好的抑菌作用。此外,Majoranaquinone在E.coli ATCC 25922菌株中表现出显著的外排泵抑制活性,并能有效抑制E.coli ATCC 25922和E.coli K-12 AG100的生物膜形成。 | |||
T35667 |
Napyradiomycin A1
Napyradiomycin A1 |
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Napyradiomycin A1is a fungal metabolite originally isolated fromC. rubraand has diverse biological activities.1,2It is active againstS. aureus,M. luteus,B. anthracis,C. bovis, andM. smegmatis(MICs = 1.56-12.5 μg/ml).1Napyradiomycin A1is an estrogen receptor antagonist (IC50= 4.2 μM in rat uterine homogenates).2It also inhibits mitochondrial NADH:ubiquinone oxidoreductase (complex I) and succinate:ubiquinone oxidoreductase (complex II) activities in bovine heart homogenates (IC50s = 20 and 9.7 μM... | |||
T36438 |
Sporogen-AO 1
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Sporogen-AO 1 is a fungal metabolite originally isolated fromA. oryzaethat has diverse biological activities.1,2,3,4,5It inhibits HIV-1 Tat transactivation in a cell-based assay with an IC50value of 15.8 μM.4Sporogen-AO 1 is cytotoxic to HeLa, KB, and NCI H187 cancer cells (IC50s = 8.3, 9, and 5.1 μM, respectively).2,5It is active againstC. albicans(MIC = 4 mM).3 1.Tanaka, S., Wada, K., Marumo, S., et al.Structure of sporogen-ao 1, a sporogenic substance of Aspergillus oryzaeTetrahedron Lett.25(... | |||
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), ... | |||
T35609 |
19-O-Acetylchaetoglobosin A
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19-O-Acetylchaetoglobosin A is a fungal metabolite originally isolated fromC. globosumthat has actin polymerization inhibitory and cytotoxic activities.1,2It inhibits actin polymerization in a cell-free assay when used at a concentration of 2 μM.219-O-Acetylchaetoglobosin A (3.2, 10, and 32 μg/ml) is cytotoxic to HeLa cervical cancer cells.1 1.Umeda, M., Ohtsubo, K., Saito, M., et al.Cytotoxicity of new cytochalasans from Chaetomium globosumExperientia31(4)435-438(1975) 2.Sekita, S., Yoshihira, ... | |||
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... | |||
T36329 |
Terpendole I
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Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 |1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Ter... | |||
T37272 |
9(S),12(S),13(S)-TriHOME
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9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME... | |||
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... | |||
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... |