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263

抑制剂 & 化合物

19

天然产物

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Cat. No. Product Name Target Signaling Pathways
T10384 Farudodstat

ASLAN003

Apoptosis; Dehydrogenase; DNA/RNA Synthesis Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
Farudodstat (ASLAN003) 是一种具有口服活性的二氢乳清酸脱氢酶 (DHODH) 抑制剂,对人 DHODH 酶的IC50为 35 nM。它通过激活 AP-1 转录因子来抑制蛋白质合成,可以诱导凋亡,并在急性髓样白血病异种移植小鼠中大大延长其生存期。
T11279 FGFR1/DDR2 inhibitor 1

Discoidin Domain Receptor (DDR); FGFR; Others Angiogenesis; Others; Tyrosine Kinase/Adaptors
FGFR1/DDR2 inhibitor 1 是一种具有口服活性的成纤维细胞生长因子受体 1 和盘状蛋白域受体 2 的抑制剂,能够抑制 FGFR1 (IC50:31.1 nM) 和 DDR2 (IC50:3.2 nM),具有抗肿瘤作用。
T12483 Piperidine-MO-1

Others Others
Piperidine-MO-1是多巴胺受体 (dopamine receptor) 调节剂,在大鼠纹状体中增加DOPAC 的 ED50 值为68 μmol/kg
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。
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。
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。
T73616 Glutamate dehydrogenase (NAD(P))

Glutamate dehydrogenase NAD(P) (GLDH)(谷氨酸脱氢酶 NAD(P))是一种存在于肝细胞、肾组织、脑、肌肉和肠细胞的线粒体酶,主要应用于生化研究。作为尿素循环的一环,该酶催化谷氨酸的逆向氧化脱氨反应,生成α-酮戊二酸(α-KG)。
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 (110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。
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。
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。
T37190 L-Allylglycine

Dehydrogenase; GABA Receptor Membrane transporter/Ion channel; Metabolism; Neuroscience
L-Allylglycine 是 GABA 合成酶(谷氨酸脱羧酶)的有效抑制剂。
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。
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。
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。
T40319 PIM-IN-1

PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC 50 = 61 nM; pS6, EC 50 = 71 nM).
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
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。
T38221 N,N-Dipropyldopamine (hydrobromide)

N,N-Dipropyldopamine is a dopamine receptor agonist.1,2,3 It decreases dihydrophenylalanine (DOPA) levels in the limbic forebrain and striatum of reserpinized rats (ED50s = 25 and 20 μmol/kg, respectively), as well as reduces homovanillic acid levels in rat striatum when administered at a dose of 80 μmol/kg.1 N,N-Dipropyldopamine (0.5-16 mg/kg) reduces spontaneous locomotor activity in mice, an effect that can be reversed by the antipsychotic spiroperidol.2,3
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。
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.
T36296 BIO5192 hydrate

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days...
T29186 YM49598

YM-49598,YM 49598

YM49598 is a tachykinin receptor antagonist. YM49598 exhibited high binding affinities at NK(1) (pK(i) = 9.09 +/- 0.02) and NK(2) (pK(i) = 9.94 +/- 0.03) receptors, respectively. YM49598 was almost inactive but produced a potent inhibition (IC(50) = 11 +/
T36254 dTAGV-1 hydrochloride

Hydrochloride salt of dTAGV-1. Suitable for use in vivo. Following ip administration of 10 mg/kg in mice: T = 4.43 h; Cmax = 2123 ng mL-1; AUCinf = 18517 hr*ng mL-1 and CL = 9.05 mL min-1 kg-1 Negative control dTAGV-1-NEG also available. Important: It is recommended that DMSO stock solutions of this compound are made and used on the same day and are not subjected to freeze/thaw.
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.
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...
T70660 Azalanstat HCl

Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered l...
T60539 KG-548

KG-548 是一种ARNT/TACC3干扰剂以及HIF-1α抑制剂。KG-548 通过 ARNT 的 PAS-B 结构域与 TACC3 竞争性结合,直接干扰ARNT/TACC3复合物的形成。ARNT 是芳基烃受体核转运蛋白,也称为 HIF-β。
T79618 M3/PDE4 modulator-1

M3/PDE4 modulator-1 (10f) 为多功能化合物,具备M3mAChR拮抗和PDE4抑制作用。于OVA大鼠模型中,M3/PDE4 modulator-1 (10-1000 nM/kg;iv) 能降低半胱氨酸嗜酸性粒细胞内流。
T36055 Nitisinone-13C6

Nitisinone-13C6

Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg/kg. Nitisinone (3 mg/kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (F...
T70661 Azalanstat mesylate

Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially...
T35521 Aflatoxin G2-13C17

Aflatoxin G2-13C17

Aflatoxin G2-13C17is intended for use as an internal standard for the quantification of aflatoxin G2by GC- or LC-MS. Aflatoxin G2is a mycotoxin that has been found inAspergillus.1It is lethal to ducklings (LD50= 2.83 mg/kg) but is non-toxic to rats when administered at a dose of 200 mg/kg.2 1.Bennett, J.W., and Klich, M.MycotoxinsClin. Microbiol. Rev.16(3)497-516(2003) 2.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins a...
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
T36543 Prostaglandin B2

PGB2

Prostaglandin B2 (PGB2) is a non-enzymatic dehydration product resulting from the treatment of PGE2 or PGA2 with strong base. It has weak agonist activity on TP receptors and can increase pulmonary blood pressure in the rabbit at relatively high doses (5 ug/kg). [1]
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。
T37791 A-971432

A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 &#181M, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 &#181M) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington’s ...
T79473 Anti-inflammatory agent 46

NO Synthase Immunology/Inflammation
Anti-inflammatory agent 46(compound 7h)是一种能够抑制一氧化氮(NO)生成的化合物,通过与iNOS低能量结合,在体内有效减缓小鼠肿胀(剂量为10 mg/kg)。
T25522 Ici 216140

m216140,Ici216140,m 216140,Ici-216140,m-216140

ICI 216140 is a GRP/bombesin receptor 2 antagonist (IC50: 2 nM in vitro). At 2 mg/kg, it can decrease bombesin-stimulated pancreatic amylase secretion in rats. At 1 mM, it has been proved to attenuate bombesin-stimulated increases in blood pressure in rat
T37114 SB 242084 dihydrochloride

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9....
T14614 Biperiden Hydrochloride

KL 373 (Hydrochloride),盐酸比哌立登

Others Others
Biperiden Hydrochloride (KL 373 Hydrochloride) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker and it is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arte
T36552 CG 4305

Prostacyclin (PGI2) is a cyclooxygenase metabolite with antithrombotic properties found in vascular endothelial cells. The half-life is short both in vivo and in vitro, ranging from 30 seconds to a few minutes. CG 4305 is a stable carbacyclic analog of PGI2 that inhibits ADP-induced platelet aggregation 25% at a concentration of 50 nM. Doses of 10 mg/kg (oral) or 1 mg/kg (intraduodenal) have been shown to prevent rabbit carotid artery thrombosis.
T35829 CC-90005

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS...
T36054 D13

D13 is an acylhydrazone antifungal.1 It is active against C. neoformans in vitro (MIC80 = 0.06 μg/ml). D13 (20 mg/kg per day, p.o.) increases survival in mouse models of C. neoformans, C. albicans, or A. fumigatus infection. |1. Lazzarini, C., Haranahalli, K., Rieger, R., et al. Acylhydrazones as antifungal agents targeting the synthesis of fungal sphingolipids. Antimicrob. Agents Chemother. 62(5), e00156-00118 (2018).
T81311 RASP-IN-1

RASP-IN-1(compound A)作为一种抗黄斑变性的亲脂性化合物,在兔视网膜中展现生物活性。通过IP途径给予小鼠14C-RASP-IN-110 mg/kg)后30分钟,测得其眼杯的最大浓度(Cmax)为14.36 μg/g。
T36404 PRLX-93936

PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM...

化合物

Farudodstat
Cat.No: T10384
Synonym: ASLAN003
Target: Apoptosis, Dehydrogenase, DNA/RNA Synthesis
FGFR1/DDR2 inhibitor 1
Cat.No: T11279
Synonym:
Target: Discoidin Domain Receptor (DDR), FGFR, Others
Piperidine-MO-1
Cat.No: T12483
Synonym:
Target: Others
(S)-Vamicamide
Cat.No: T35033L
Synonym: (S)-Vamicamide (Iso-132373-81-0)
Target: AChE
KR-32568
Cat.No: T36569
Synonym:
Target: Sodium Channel
BIBB 515
Cat.No: T4039
Synonym:
Target: Others
Glutamate dehydrogenase (NAD(P))
Cat.No: T73616
Synonym:
Target:
Litoxetine
Cat.No: T67956
Synonym:
Target: 5-HT Receptor
CS 2100
Cat.No: T22697
Synonym: 1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid
Target: S1P Receptor
RO1138452
Cat.No: T4436
Synonym: CAY10441
Target: Others, Prostaglandin Receptor
CCG-203971
Cat.No: T4306
Synonym: CCG203971
Target: Rho, Ras
Unifiram
Cat.No: T38192
Synonym:
Target: Others
MTP 131 acetate
Cat.No: T35689
Synonym:
Target: Others
CP-609754
Cat.No: T38050
Synonym:
Target: Transferase
ARN-21934
Cat.No: T36968
Synonym:
Target: Topoisomerase
COR659
Cat.No: T36520
Synonym:
Target: Cannabinoid Receptor, GABA Receptor
L-Allylglycine
Cat.No: T37190
Synonym:
Target: Dehydrogenase, GABA Receptor
4-Deoxypyridoxine hydrochloride
Cat.No: T38294
Synonym:
Target: S1P Receptor
Niaprazine
Cat.No: T36949
Synonym:
Target: 5-HT Receptor, Adrenergic Receptor, Histamine Receptor
DMU-212
Cat.No: T36674
Synonym:
Target: Apoptosis, ERK
PIM-IN-1
Cat.No: T40319
Synonym:
Target:
ONO-0300302
Cat.No: T28245
Synonym: ONO 0300302
Target:
Thiacloprid
Cat.No: T38272
Synonym:
Target: AChR, Parasite
N,N-Dipropyldopamine (hydrobromide)
Cat.No: T38221
Synonym:
Target:
E2730
Cat.No: T79399
Synonym:
Target: GABA Receptor
BJ-2302
Cat.No: T70344
Synonym:
Target:
BIO5192 hydrate
Cat.No: T36296
Synonym:
Target:
YM49598
Cat.No: T29186
Synonym: YM-49598,YM 49598
Target:
dTAGV-1 hydrochloride
Cat.No: T36254
Synonym:
Target:
AM-6761
Cat.No: T26610
Synonym: AM 6761,AM6761
Target:
PI3Kα-IN-4
Cat.No: T35527
Synonym: PI3Kα-IN-4
Target:
Azalanstat HCl
Cat.No: T70660
Synonym:
Target:
KG-548
Cat.No: T60539
Synonym:
Target:
M3/PDE4 modulator-1
Cat.No: T79618
Synonym:
Target:
Nitisinone-13C6
Cat.No: T36055
Synonym: Nitisinone-13C6
Target:
Azalanstat mesylate
Cat.No: T70661
Synonym:
Target:
Aflatoxin G2-13C17
Cat.No: T35521
Synonym: Aflatoxin G2-13C17
Target:
J-104132
Cat.No: T27647
Synonym: L753037,L 753037,J104132,J 104132,L-753037
Target:
Prostaglandin B2
Cat.No: T36543
Synonym: PGB2
Target:
CGP 37849
Cat.No: T7720
Synonym: CGP-37849,CGP37849
Target: NMDAR, iGluR
A-971432
Cat.No: T37791
Synonym:
Target:
Anti-inflammatory agent 46
Cat.No: T79473
Synonym:
Target: NO Synthase
Ici 216140
Cat.No: T25522
Synonym: m216140,Ici216140,m 216140,Ici-216140,m-216140
Target:
SB 242084 dihydrochloride
Cat.No: T37114
Synonym:
Target:
Biperiden Hydrochloride
Cat.No: T14614
Synonym: KL 373 (Hydrochloride),盐酸比哌立登
Target: Others
CG 4305
Cat.No: T36552
Synonym:
Target:
CC-90005
Cat.No: T35829
Synonym:
Target:
D13
Cat.No: T36054
Synonym:
Target:
RASP-IN-1
Cat.No: T81311
Synonym:
Target:
PRLX-93936
Cat.No: T36404
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5S1889 Yunaconitine

Guayewuanine B,滇乌头碱

Others Others
Yunaconitine (Guayewuanine B) 是一种乌头类生物碱,具有剧毒。
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。
T5S0636 Citric acid

柠檬酸,Citro,Citretten

Apoptosis; Others; Endogenous Metabolite; Antibacterial; Antibiotic Apoptosis; Metabolism; Microbiology/Virology; Others
Citric acid (Citro) 是柑橘类水果中发现的弱有机三羧酸。柠檬酸是食品添加剂和天然防腐剂。
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。
T4S21320 ISOGINKGETIN

异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮

MMP; Others Others; Proteases/Proteasome
ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂,也是一种Pre-mRNA Splicing 抑制剂。
T2S2215 Crebanine

Apoptosis; Others; Akt Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
Crebanine 是来自于韦诺萨千金藤的一种生物碱,通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性,还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。
T35624 Ajoene

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 &#181g/ml) and Gram-negative bacteria (MICs = 136-200 &#181g/ml), as well as yeasts (MICs = 10-20 &#181g/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 &#181M), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 &#181M).2It reduces...
T83903 Polymyxin B2 sulfate

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。
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 ...
T83915 Norbixin hydrate

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0.11 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。
T36179 Aspulvinone O

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...
T36227 Beauveriolide III

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 ...
T35750 Trypacidin

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

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...
T35751 Violacein

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 &#181M, respectively). It is also active aga...
T36749 Herboxidiene

Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herbo...
T35779 Oosporein

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

(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

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...

天然产物

Yunaconitine
Cat.No: T5S1889
Synonym: Guayewuanine B,滇乌头碱
Target: Others
Crotonoside
Cat.No: T6S0033
Synonym: 巴豆苷;异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE
Target: Others, FLT, HDAC
Citric acid
Cat.No: T5S0636
Synonym: 柠檬酸,Citro,Citretten
Target: Apoptosis, Others, Endogenous Metabolite, Antibacterial, Antibiotic
Artemitin
Cat.No: TCS1704
Synonym: 艾黄素,Artemetin,Artemisetin,Erianthin
Target: Antioxidant
ISOGINKGETIN
Cat.No: T4S21320
Synonym: 异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮
Target: MMP, Others
Crebanine
Cat.No: T2S2215
Synonym:
Target: Apoptosis, Others, Akt
Ajoene
Cat.No: T35624
Synonym:
Target:
Polymyxin B2 sulfate
Cat.No: T83903
Synonym:
Target:
Cardamonin
Cat.No: T66078
Synonym:
Target:
Norbixin hydrate
Cat.No: T83915
Synonym:
Target:
Aspulvinone O
Cat.No: T36179
Synonym:
Target:
Beauveriolide III
Cat.No: T36227
Synonym:
Target:
Trypacidin
Cat.No: T35750
Synonym:
Target:
(rel)-Asperparaline A
Cat.No: T37609
Synonym:
Target:
Violacein
Cat.No: T35751
Synonym:
Target:
Herboxidiene
Cat.No: T36749
Synonym:
Target:
Oosporein
Cat.No: T35779
Synonym:
Target:
(E)-Ajoene
Cat.No: T36448
Synonym:
Target:
Nemorosone
Cat.No: T36954
Synonym:
Target:
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