271
38
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6847 |
GSK-J1
GSK J1 |
Histone Demethylase | Chromatin/Epigenetic |
GSK-J1 是一种高效的 H3K27 组蛋白去甲基化酶抑制剂,在无细胞试验中对 JMJD3 (KDM6B) 和 UTX (KDM6A) 的 IC50 分别为 28 nM 和 53 nM,比其他测试的去甲基化酶选择性高 10 倍以上。 | |||
T2272 |
BPR1J-097
BPR1J097 |
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
BPR1-J097 是新型的、强效的FLT3抑制剂 (IC50:11 nM)。 | |||
T4261 |
BPR1J-097 hydrochloride (1327167-19-0(free base))
|
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
BPR1J-097 hydrochloride (1327167-19-0(free base)) 是一种新型小分子 FLT-3抑制剂(IC50=11±7 nM),具有很好的体内抗肿瘤活性。 | |||
T8884 |
hSMG-1 inhibitor 11j
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
hSMG-1 inhibitor 11j 是一种嘧啶衍生物,是有效的和选择性的 hSMG-1 抑制剂,IC50 为 0.11 nM。hSMG-1 inhibitor 11j 对 hSMG-1 的选择性是 mTOR (IC50=50 nM),PI3Kα/γ (IC50=92/60 nM) 和 CDK1/CDK2 (IC50=32/7.1 μM) 的 455 倍以上。hSMG-1 inhibitor 11j 可用于癌症研究。 | |||
T33281 |
Melflufen
Prodrug J-1, Melflufen, Melphalan flufenamide,Melphalan flufenamide,J 1,J1,J-1 |
||
Melphalen fluoroaniline, also known as melphalen, J-1, or prodrug J-1, is a prodrug of melphalen, in which the alkylating agent melphalen is combined with fluoroaniline and has potential antitumor and antiangiogenic activities. | |||
T11475 |
GSK-J1 lithium salt
|
Histone Demethylase | Chromatin/Epigenetic |
GSK-J1 lithium salt 是一种有效的 H3K27me3/me2-去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 的抑制剂,对 KDM6B 的 IC50值为 60 nM。 | |||
T68836 |
ADS-J1
|
||
ADS-J1 is an HIV-1 entry inhibitor that potently inhibits seminal amyloid fibrillization and block fibril-mediated enhancement of viral infection. Semen-derived amyloid fibrils, comprising SEVI (semen-derived enhancer of viral infection) fibrils and SEM1 fibrils, may remarkably enhance HIV-1 sexual transmission and are potential targets for the development of an effective microbicide. | |||
T71916 |
GSK-J1 sodium salt
|
||
GSK-J1 sodium salt is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX. | |||
T70779 |
BPR1J-340
|
||
BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD(+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibit... | |||
T63903 | BPR1J-097 Hydrochloride | ||
BPR1J-097 Hydrochloride 是新型的、强效的 FLT3 抑制剂 (IC50: 11 nM)。 | |||
T3068 |
AT9283
J-504568 |
Apoptosis; FLT; JAK; Bcr-Abl; Aurora Kinase; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
AT9283 (J-504568) 是一种多靶点激酶抑制剂,抑制多种实体瘤在体内外的生长和存活,有效抑制Aurora A/B,JAK2/3,Abl (T315I),和Flt3,IC50值范围为 1-30 nM。 | |||
T35610 |
2,5-dimethyl Celecoxib
|
Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells |
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。 | |||
T38240 |
2,6-Dichlorodiphenylamine
|
Antibacterial | Microbiology/Virology |
2,6-Dichlorodiphenylamine 是双氯芬酸钠的一种结构类似物,显示出抗白色念珠菌活性。2,6-Dichlorodiphenylamine 是非选择性抗炎剂,为COX 的抑制剂,在 CHO 细胞中,对人 COX-1 和 COX-2 的IC50分别为 4 和 1.3 nM。 | |||
T37149 |
Carbamazepine 10,11-epoxide
|
Others | Others |
Carbamazepine 10,11-epoxide 是抗惊厥药卡马西平 (carbamazepine) 的活性代谢物。它由卡马西平通过微粒体中的细胞色素 P450 (CYP) 同种型 CYP3A4 和 CYP2C8 形成,微粒体分别由表达 CYP3A4 或 CYP2C8 的 HepG2 细胞制备。它对小鼠电击诱发的癫痫发作具有抗惊厥活性。 | |||
T35689 |
MTP 131 acetate
|
Others | Others |
MTP 131 acetate 是一种小的线粒体靶向四肽。 | |||
T35841 |
5-Benzyloxygramine
|
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
5-Benzyloxygramine 是一种 N 蛋白、蛋白互作的原位稳定剂,具有抗病毒和稳定 N-NTD 蛋白的作用。它能够阻断多巴胺受体,可拮抗 5-HT 对大鼠子宫和兔耳的作用。 | |||
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。 | |||
T36083 |
DS-7423
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
DS-7423 是PI3K 和mTOR 的有效抑制剂,抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。 | |||
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。 | |||
T36141 |
Boscalid
|
Mitochondrial Metabolism | Metabolism |
Boscalid 是一种广谱羧酰胺类杀菌剂,通过与线粒体复合物 II/琥珀酸脱氢酶的泛醌位点结合来抑制真菌呼吸。 | |||
T73802 | (S,S)-J-113397 | ||
(S,S)-J-113397 是 J-113397 的异构体。J-113397 是一种阿片类受体 (Opioid Receptor) 拮抗剂。 | |||
T36944 |
Ara-G
|
Nucleoside Antimetabolite/Analog | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Ara-G 是一种脱氧鸟苷 (GdR) 类似物和核苷类似物,可被 T 淋巴谱系细胞迅速转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸 (araGTP),从而抑制 DNA 合成和对 T 淋巴母细胞的选择性体外毒性细胞系以及来自 T 细胞急性淋巴细胞白血病 (ALL) 患者的新鲜分离的白血病细胞。 | |||
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。 | |||
T27647 |
J-104132
L753037,L 753037,J104132,J 104132,L-753037 |
||
J-104132 is a potetn and selective endothelin A/B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ova | |||
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。 | |||
T82984 |
Aplithianines A
|
PKA | Tyrosine Kinase/Adaptors |
Aplithianines A,一种J-PKAcα抑制剂,表现出1 μM的IC50,同时对于野生型PKA,IC50值达到84 nM。该化合物通过与ATP口袋的竞争性结合来抑制J-PKAcα的催化作用。 | |||
T21999 |
(±)-J 113397
|
||
(±)-J-113397 是一种有效的、高选择性的非肽基ORL1 受体拮抗剂,对人克隆 ORL1 的Ki 为 1.8 nM。在体外,J-113397 抑制 nociceptin/orphanin FQ 刺激的GTPγS 与表达 ORL1 的 CHO 细胞结合,IC50值为 5.3 nM。J-113397 可用于研究 nociceptin/orphanin FQ 的生理作用。 | |||
T80907 |
TYVPANASL
|
||
TYVPANASL为由HER2/neu的9个氨基酸组成的MHC I结合CD8 T细胞表位,可用于制备J-LEAPS疫苗。 | |||
T125649 |
Cyclocarioside J
|
||
Cyclocarioside J 是一种有用的有机化合物,可用于生命科学领域的相关研究。其产品编号为 T125649,CAS号为 1644624-86-1。 | |||
T80906 |
TYVPANASL TFA
|
||
TYVPANASL TFA,一种由HER2/neu的9个氨基酸组成,可结合MHC I并与CD8 T细胞表位相关的化合物。该化合物可用于制备J-LEAPS疫苗。 | |||
T78790 | J-1048 | ||
J-1048 是一种专门针对激活素受体样激酶 5 (ALK5) 的抑制剂,能够有效地通过抑制 TGF-β/Smad 信号通路来防止 TAA 诱导的小鼠肝纤维化。 | |||
T38233 |
Hexanoyl-L-carnitine (chloride)
|
||
Hexanoyl-L-carnitine is a medium-chain acylcarnitine. It has been used in the synthesis of acylcarnitine benzyl esters.1 1.Gong, X.-w., Li, J.-p., Wu, J.-f., et al.Synthesis of carnitine benzyl esters as prodrugsJ. Chem. Res.2008(6)327-330(2008) | |||
T37107 |
Bz-rA Phosphoramidite
|
||
Bz-rA Phosphoramidite is used for ribonucleotides modification[1]. [1]. Elise Malek-Adamian, et al. 4'-C-Methoxy-2'-deoxy-2'-fluoro Modified Ribonucleotides Improve Metabolic Stability and Elicit Efficient RNAi-Mediated Gene Silencing. J Am Chem Soc. 2017 Oct 18;139(41):14542-14555. | |||
T83357 |
3-Hydroxy-2-(palmitoyloxy)propyl stearat
|
||
3-Hydroxy-2-(palmitoyloxy)propyl stearate是一种从棕色巨藻Fucus virsoides J. Agardh的极性较小部分分离得到的非挥发性化合物。该化合物具有良好的自由基清除能力,并能保护斑马鱼胚胎免受过氧化氢诱导的氧化应激。 | |||
T36022 |
Fluticasone 17β-Carboxylic Acid
|
||
Fluticasone 17β-carboxylic acid is an intermediate in the synthesis of the glucocorticosteroid fluticasone propionate .1References1. Zhou, J., Jin, C., and Su, W. Improved synthesis of fluticasone propionate. Org. Process Res. Dev. 18(8), 928-933 (2014). Fluticasone 17β-carboxylic acid is an intermediate in the synthesis of the glucocorticosteroid fluticasone propionate .1 References1. Zhou, J., Jin, C., and Su, W. Improved synthesis of fluticasone propionate. Org. Process Res. Dev. 18(8), 928-9... | |||
T81940 |
Lepunafusp alfa
JR-171 |
||
Lepunafusp alfa (JR-171) 是一款由 J-Brain Cargo 和 IDUA (α-L-艾杜糖苷酶,溶酶体酶) 构成的血脑屏障透过性融合蛋白。该融合蛋白能有效降低硫酸乙酰肝素 (HS) 与硫酸皮肤素 (DS) 浓度,适合作为 I 型粘多糖贮积症研究用途。 | |||
T37176 |
Edoxaban impurity 6
|
||
Edoxaban impurity 6 is an impurity of Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention[1][2]. [1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9.[2]. Mendell J, Lee F, Chen S, The Effe... | |||
T36379 |
Halometasone
|
||
Halometasone is a synthetic corticosteroid.1,2Formulations containing halometasone have been used in the treatment of psoriasis vulgaris and eczematous dermatoses. 1.de la Brassine, M., Kint, A., Lachapelle, J.M., et al.Halomethasone (C 48.401-Ba) for the topical treatment of common dermatosesJ. Int. Med. Res.12(5)307-309(1984) 2.Zhu, J.-W., Wu, X.-J., Lu, Z.-F., et al.Role of VEGF receptors in normal and psoriatic human keratinocytes: Evidence from irradiation with different UV sourcesPLoS One8... | |||
T35873 |
C19 Ceramide (d18:1/19:0)
C19 Ceramide (d18:1/19:0) |
||
C19 Ceramide is a naturally occurring ceramide that has been found in J. juncea extracts as well as rat brain and mouse heart.[1],[2],[3] It is elevated in adult and decreased in juvenile whole rat brain extracts by 114 and 37%, respectively, following chronic ethanol exposure.[2] C19 Ceramide is also increased in mouse hearts following administration of angiotensin II.[3] | |||
T68363 |
OUN10989
|
||
OUN10989, an analogue compound of LP-261, is a Potent Antimitotic Agent. OUN10989 exhibited potent inhibition of mitosis at the G2/M stage. OUN10989 was first reported in J. Med. Chem 54(1), 179-200; 2011 (compound 7). This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming). | |||
T38323 |
A-943931 (hydrochloride hydrate)
|
||
A-943931 is a histamine H4receptor antagonist (Ki= 3.8 nM).1In vivo, A-943931 inhibits scratching induced by clobenpropit in mice (ED50= 26 μmoles/kg, i.p.). 1.Milicic, I., Witte, D.G., Miller, T.L., et al.Identification of two potent and selective histamine H4 receptor antagonists with antipruritic activityFASEB J.23(S1)760.768-760.768(2009) | |||
T37297 |
Ru360
|
||
Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial ce... | |||
T35686 |
3-Acetyl Betulinaldehyde
|
||
3-Acetyl betulinaldehyde is a triterpene and derivative of the cholesterol biosynthesis inhibitor betulin that has been found inA. japonica.1It is an intermediate in the synthesis of 3-acetylbetulinic acid, as well as various lupine and germanicane triterpenes and saponins with anticancer activity.2 1.Tung, N.H., Kwon, H.-J., Kim, J.-H., et al.An anti-influenza component of the bark of Alnus japonicaArch. Pharm. Res.33(3)363-367(2010) 2.Thibeault, D., Gauthier, C., Legault, J., et al.Synthesis a... | |||
T37349 |
Cymoxanil
|
||
Cymoxanil is a fungicidal against plant diseases caused by fungi belonging to the Perenosporales[1]. [1]. Frederique Tellier , et al. Characterization of Metabolites of Fungicidal Cymoxanil in a Sensitive Strain of Botrytis Cinerea. J Agric Food Chem. 2008 Sep 10;56(17):8050-7. | |||
T37516 |
[(3R)-3-Hydroxydodecanoyl]-L-carnitine
|
||
[(3R)-3-Hydroxydodecanoyl]-L-carnitine is an endogenous metabolite[1]. [1]. Hunter WG, et al. Metabolomic Profiling Identifies Novel Circulating Biomarkers of Mitochondrial Dysfunction Differentially Elevated in Heart Failure With Preserved Versus Reduced Ejection Fraction: Evidence for Shared Metabolic Impairments in Clinical Heart Failure. J Am Heart Assoc. 2016;5(8):e003190. Published 2016 Jul 29. | |||
T36225 |
N-p-Tosyl-Gly-Pro-Lys-pNA (acetate)
|
||
N-p-Tosyl-Gly-Pro-Lys-pNA is a colorimetric substrate for plasmin.1,2,3Plasmin binds and hydrolyzes N-p-tosyl-Gly-Pro-Lys-pNA to releasep-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of plasmin activity. 1.Jespersen, J., Gram, J., and Astrup, T.The autodigestion of human plasmin follows a bimolecular mode of reaction subject to product inhibitionThromb. Res.41(3)395-404(1986) 2.Kim, S.H., and Choi, N.S.Electrophoretic analysis of protease inhibitor... | |||
T38288 |
Profenofos
|
||
Profenofos is an acetylcholinesterase-inhibiting organophosphorus pesticide on field crops, vegetables, and fruit crops [1]. [1]. Madhulika Kushwaha, et al. Kushwaha, M., et al.. Profenofos, an Acetylcholinesterase-Inhibiting Organophosphorus Pesticide: A Short Review of Its Usage, Toxicity, and Biodegradation. J Environ Qual.2016 Sep;45(5):1478-1489. | |||
T37140 |
5'-O-DMT-rI
|
||
5’-O-DMT-Ri can be used in the synthesis of oligoribonucleotides[1]. [1]. Kadokura M. Synthesis of 4-thiouridine, 6-thioinosine, and 6-thioguanosine 3’,5’-O-bisphosphates as donor molecules for RNA ligation and their application to the synthesis of photoactivatable TMG-capped U1 snRNA fragments. J Org Chem. 2000 Aug 25;65(17):5104-13. | |||
T36679 |
Rp-cAMPS sodium salt
|
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Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6]. A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic t... | |||
T78053 |
PD-L1-IN-2
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PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
"PD-L1-IN-2是一种具有潜力的肿瘤免疫治疗剂,具有抑制PD-L1的活性。该化合物为Naamidine J的衍生物,可通过降低体内PD-L1的表达并增强肿瘤浸润性T细胞的免疫反应来发挥抗肿瘤效果。PD-L1-IN-2主要应用于结直肠癌的研究领域。" |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S2115 |
Ginkgolide J
BN 52024,7-beta-Hydroxyginkgolide A,银杏内酯 J,银杏内酯J |
PDE | Metabolism |
Ginkgolide J (BN 52024) 是一种银杏叶中非黄酮部分的主要成分(IC50:12-54 µM),具有神经保护和抗神经元凋亡功能。 | |||
T37709 |
2,2,2-Trichloroethanol
|
Potassium Channel; Endogenous Metabolite | Membrane transporter/Ion channel; Metabolism |
2,2,2-Trichloroethanol 是非经典的 K2P 通道 TREK-1和 TRAAK 的激动剂。 | |||
T79955 |
Schiarisanrin A
Kadsulignan J |
NO Synthase | Immunology/Inflammation |
Schiarisanrin A (Kadsulignan J) 作为一种木脂素,具有对 BV-2 细胞中 NO 产生的抑制活性,其IC50值为 9.6 μM。 | |||
TMA2282 |
Caesalpin J
|
Others | Others |
Caesalpin J 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 TMA2282,CAS号为 99217-67-1。 | |||
T81178 |
Senkyunolide J
|
||
Senkyunolide J为川芎根茎中提取的邻苯二酸酯类化合物。 | |||
T75558 | Bruceine J | ||
Bruceine J 是一种类黄酮,是一种天然产物,可以从Br. jaVanica 的果实中分离得到。Bruceine J 具有抗巴贝斯活性。 | |||
T75504 | Xanthine oxidase-IN-8 | ||
Xanthine oxidase-IN-8 (Icarisids J) (Compound 7) 是一种 XOD 抑制剂,IC50值为 29.71 μM。 | |||
T75479 | Guignardone J | ||
Guignardone J 是从内生真菌 Phyllosticta capitalensis 中分离出的次级代谢产物。 | |||
TN5635 |
Gancaonin J
|
||
Gancaonin J 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 TN5635,CAS号为 129280-37-1。 | |||
T75530 | Nardoguaianone J | ||
Nardoguaianone J,一种愈创木脂类化合物,可从Nardostachys chinensis 的根中分离得到。Nardoguaianone J 可提高SERT 活性。 | |||
T79935 |
Forrestiacids J
|
ATP Citrate Lyase | Metabolism |
Forrestiacids J为一种特异性抑制ATP-柠檬酸裂解酶 (ACL) 的化合物,其IC50值为2.6 μM。 | |||
T81482 |
Physagulide J
|
||
Physagulide J, 一种睡茄内酯类化合物,可从苦蘵 (Physalis angulata L.) 分离。此化合物与苦蘵的其他活性成分共同展现抗炎及抗肿瘤活性。 | |||
T82287 |
Glycoside St-J
|
||
Glycoside St-J(Compound 2)为一种三萜皂苷,具备抑制HeLa细胞增殖的抗肿瘤活性,源自天然银莲花提取。该化合物适用于开发新型抗癌药物的研究。 | |||
T75475 | Chaetosemin J | ||
Chaetosemin J,一种对植物病原真菌(如灰霉病菌、番茄交链孢菌、稻瘟病菌和赤霉素)具有抑制活性的抗真菌代谢产物,MIC值在12.5-25 μM范围内。 | |||
T37451 |
Stachybotrysin B
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Stachybotrysin B is a fungal metabolite originally isolated from S. chartarum and has antiviral and anticancer activities.1,2 It has antiviral activity against HIV in SupT1 cells (IC50 = 19.2 μM).1 Stachybotrysin B is cytotoxic to K562, HeLa, and HL-60 cells (IC50s = 21.72, 39.63, and 18.5 μM, respectively).2 |1. Zhao, J., Feng, J., Tan, Z., et al. Stachybotrysins A-G, phenylspirodrimane derivatives from the fungus Stachybotrys chartarum. J. Nat. Prod. 80(6), 1819-1826 (2017).|2. Ma, X.-h., Zhen... | |||
T36295 | Echistatin TFA | ||
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1[1][2][3][4]. [1]. J Musial, et al. Inhibition of platelet adhesion to surfaces of extracorporeal circuits by disintegrins. RGD-containing peptides from viper venoms. Circulation. 1990 Jul;82(1):261-73.[2]. ... | |||
T36000 |
3-Hydroxyterphenyllin
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3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methi... | |||
T37690 |
Phenylpyropene A
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Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of ... | |||
T36734 |
Methyl brevifolincarboxylate
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Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A/Puerto Rico/8/34 (H1N1) and A/Aichi/2/68 (H3N2) with IC50s of 27.16 μM and 33.41 μM. Anti-oxidant activity[1][2]. Methyl brevifolincarboxylate exhibits significant DPPH radical scavenging activity with an IC50 value of 8.9 μM. [1]. Wu QY, et al. Chromatographic fingerprint and the simultane... | |||
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... | |||
T36893 |
4-oxo Withaferin A
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4-oxo Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells and carboplatin-resistant A2780 (A2780/CP70) cells (IC50s = 7.3 and <1 μM, respectively) and is 4.4-fold selective for A2780 cells over non-cancerous ARPE19 cells.References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian ca... | |||
T36915 |
21-Deoxycortisol
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21-Deoxycortisol is a corticosteroid metabolite of 17-hydroxyprogesterone produced in the adrenal glandvia11-hydroxylation by 11β-hydroxylase.1,2Serum levels of 21-deoxycortisol are elevated in patients with congenital adrenal hyperplasia that are heterozygous for mutations inCYP2A21, the gene encoding steroid 21-hydroxylase, and have been used as a biomarker for the detection of 21-hydroxylase deficiencies. 1.Fiet, J., Villette, J.-M., Galons, H., et al.The application of a new highly-sensitive... | |||
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... | |||
T35647 |
4-oxo-27-TBDMS Withaferin A
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4-oxo-27-TBDMS Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells (IC50 = 17 μM) but not to carboplatin-resistant A2780 (A2780/CP70) cells (IC50 = >100 μM). It is selective for A2780 cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780 cells.References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of wi... | |||
T37876 |
Fengycin
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Fengycin is a cyclic lipopeptide used as an agricultural fungicide. Fengmycin has an anti-fungal infection effect by damaging the target’s cell membrane[1]. [1]. Sreyoshi Sur, et al. Selectivity and Mechanism of Fengycin, an Antimicrobial Lipopeptide, from Molecular Dynamics. J Phys Chem B. 2018 Mar 1;122(8):2219-2226. | |||
T35911 |
Piliformic Acid
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Piliformic acid is a fungal metabolite that has been found inN. pseudotrichiaand has diverse biological activities.1,2It is cytotoxic to BC-1 human breast cancer cells (IC50= 5 μg/ml).2Piloformic acid is active againstL. braziliensisamastigotes (IC50= 78.5 μM). It is also active against the plant pathogenic fungiC. gloeosporioides(MIC = 292 μM).1 1.Elias, L.M., Fortkamp, D., Sartori, S.B., et al.The potential of compounds isolated from Xylaria spp. as antifungal agents against anthracnoseBraz. J... | |||
T35741 |
Gliovirin
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Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decrease... | |||
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... | |||
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... | |||
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(... | |||
T38330 |
Collinin
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Collinin is a coumarin that has been found in Z. schinifolium and has diverse biological activities.1,2,3,4 It is active against drug-susceptible and -resistant strains of M. tuberculosis (MIC50s = 3.13-6.25 μg/ml).1 Collinin inhibits LPS-induced nitric oxide (NO) production (IC50 = 5.9 μM) and reduces COX-2 protein levels in RAW 264.7 cells.2 It completely inhibits aggregation of isolated rabbit platelets induced by arachidonic acid , collagen, or platelet activating factor (PAF) when used at a... | |||
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... | |||
T36563 |
(E)-Guggulsterone
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Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hy... | |||
T35415 |
α-D-Glucose-1,6-bisphosphate (potassium salt hydrate)
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α-D-Glucose-1,6-bisphosphate is abis-phosphorylated derivative of α-D-glucose that has roles in carbohydrate metabolism.1It is the product of the reaction of glucose-1- or 6-phosphate with glucose-1,6-bisphosphate synthase (PGM2LI) in the conversion of 1,3-bisphosphoglycerate to 3-phosphoglycerate.2It is also a cofactor for the bacterial enzyme phosphopentomutase.3,4α-D-Glucose-1,6-bisphosphate has been used in the study of carbohydrate metabolism. 1.Beitner, R.Regulation of carbohydrate metabol... | |||
T36348 |
Cerebroside C
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Cerebroside C is a fungal metabolite and glycosphingolipid that has been found in the rice pathogenic fungusM. grisea.1It induces production of the phytoalexin momilactone A when applied to wounded rice leaves, indicating that cerebroside C is an elicitor of the hypersensitive response in rice. Cerebroside C increases germination rate and reduces germination time in wheat seeds in a concentration-dependent manner at 4°C.2It also increases root length, fresh weight, and dry weight of wheat seedli... | |||
T37452 |
Stephacidin B
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Stephacidin B is a fungal metabolite that has been found inA. ochraceus.1Dimeric stephacidin B is rapidly converted to a monomer, avrainvillamide ,in vitro.2Stephacidin B is cytotoxic to a variety of cancer cells, including testosterone-independent PC3 and -sensitive LNCaP prostate cancer cells (IC50s = 0.37 and 0.06 μM, respectively) and estradiol-independent SK-BR-3 and -sensitive MCF-7 breast cancer cells (IC50s = 0.32 and 0.27 μM, respectively).1It induces apoptosis in HepG2 and Huh7 hepatoc... | |||
T38069 |
Aquastatin A
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Aquastatin A is a fungal metabolite originally isolated fromF. aquaeductuumthat has diverse biological activities.1It is active againstS. aureus(MIC = 32 μg/ml) and inhibits enoyl-acyl carrier protein reductase (Fabl; IC50= 3.2 μM) andS. aureusfatty acid synthesis (IC50= 3.5 μM).2Aquastatin A also inhibits the Na+/K+-ATPase and H+/K+-ATPase (IC50s = 7.1 and 6.2 μM, respectively), as well as protein tyrosine phosphatase 1B (PTP1B; IC50= 0.19 μM).1,3 1.Hamano, K., Kinoshita-Okami, M., Minagawa, K.... | |||
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), ... |