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35

抑制剂 & 化合物

20

天然产物

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Cat. No. Product Name Target Signaling Pathways
T12341 P-gp inhibitor 1

Others; P-gp Membrane transporter/Ion channel; Neuroscience; Others
P-gp inhibitor 1 抑制逆转 P-糖蛋白介导的多药耐药性,EC50 为 57.9 nM(K562/A02 细胞)。
T11071 Dofequidar fumarate

MS-209

P-gp Membrane transporter/Ion channel; Neuroscience
Dofequidar fumarate (MS-209) 是口服活性的喹啉化合物,通过抑制 ABCB1/P-gp 和 ABCC1/MDR 相关蛋白 1 来克服 MDR
T16561 Polyoxyethylene stearate

POES,聚氧乙烯硬脂酸酯

Antibacterial; P-gp Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
Polyoxyethylene stearate (POES) 是一种非离子乳化剂。
T8426 Encequidar

HM30181,HM30181A

P-gp Membrane transporter/Ion channel; Neuroscience
Encequidar (HM30181A) 是一种选择性 P-糖蛋白抑制剂。
T6287 Tariquidar

XR9576,他立喹达

P-gp Membrane transporter/Ion channel; Neuroscience
Tariquidar (XR9576) 是一种特异性有效的P-糖蛋白抑制剂,Kd 为 5.1 nM。
T4059 Selamectin

UK-124114,司拉克丁,塞拉菌素

Chloride channel; P-gp; Parasite Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
Selamectin (UK-124114) 是半合成的大环内酯,是一种驱虫剂,可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。它还是抗寄生虫剂,可激活神经元和咽肌中的谷氨酸门控氯离子通道,以预防恶丝虫,淋巴丝虫和线虫感染。它还是 P-糖蛋白底物和抑制剂,IC50为 120 nM。
T0351 Risperidone

Risperidal,R 64 766,利培酮

Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; P-gp GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
Risperidone (R 64 766) 是5-HT2受体阻断剂、P-糖蛋白抑制剂和多巴胺 D2受体的拮抗剂,对 5-HT2A 和多巴胺 D2受体的 Ki 值分别为 4.8 和 5.9 nM。
T11578L Encequidar mesylate

HM30181 mesylate,HM30181A mesylate

P-gp Membrane transporter/Ion channel; Neuroscience
Encequidar mesylate (HM30181A mesylate) 是竞争性有效的 P-糖蛋白抑制剂。
T13383 Zamicastat

BIA 5-1058

BCRP; Hydroxylase; P-gp Membrane transporter/Ion channel; Metabolism; Neuroscience
Zamicastat (BIA 5-1058) 是多巴胺 β-羟化酶 (DBH) 抑制剂,可透过血脑屏障引起中枢和周边效应,具有降血压作用。它也是一种浓度依赖性的双重 P-gp 和 BCRP 抑制剂,IC50值分别为 73.8 和 17.0 μM。
T8389 Trifluoperazine

三氟拉嗪,trifluoroperazine

CaMK; Dopamine Receptor; Influenza Virus; Adrenergic Receptor; P-gp; Autophagy Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
Trifluoperazine (trifluoroperazine) 是一种多巴胺 D2 受体抑制剂,可治疗精神分裂症。它是NUPR1抑制剂,具有抗癌活性。它是α1-adrenergic 受体拮抗剂,是流感病毒形态发生的可逆抑制剂。
T1634 Glibenclamide

格列本脲,Glyburide

Potassium Channel; Mitochondrial Metabolism; CFTR; P-gp; Autophagy Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience
Glibenclamide (Glyburide) 是一种具有口服活性的 ATP 敏感的 K+通道抑制剂,可研究糖尿病和肥胖。它抑制 P-糖蛋白,可直接结合并阻断 KATP 的 SUR1亚基并抑制囊性纤维化跨膜传导调节蛋白。它通过诱导膜离子通透性干扰线粒体生物能,可诱导自噬。
T0100L Atazanavir

Zrivada,Reyataz,Latazanavir,阿扎那韦,BMS-232632

P450; SARS-CoV; HIV Protease; P-gp Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
Atazanavir (BMS-232632) 是一种高选择性的HIV-1蛋白酶抑制剂,可研究艾滋病毒感染。它也是SARS-CoV 3CLpro 的抑制剂,IC50为 3.49 μM。它是CYP3A4的底物和抑制剂,也是P-糖蛋白的抑制剂和诱导剂。
T20656 Verapamil

NSC 135784,维拉帕米,NSC-135784,CP-16533-1,(±)-Verapamil

P450; Calcium Channel; P-gp Membrane transporter/Ion channel; Metabolism; Neuroscience
Verapamil (CP-16533-1) 是一种钙通道阻滞剂,是一种口服有效的 P-gp 抑制剂。Verapamil 抑制 CYP3A4,可用于治疗高血压、心律失常和心绞痛的研究。
T16339 Norverapamil hydrochloride

(±)-Norverapamil hydrochloride,D591 hydrochloride,盐酸去甲维拉帕米

Calcium Channel; P-gp; Drug Metabolite Membrane transporter/Ion channel; Metabolism; Neuroscience
Norverapamil hydrochloride (D591 hydrochloride) 是 Verapamil 的 N-去甲基代谢物,是 L 型钙通道阻滞剂和 P-糖蛋白 (P-gp) 功能抑制剂。
T1010 Verapamil hydrochloride

Manidon,盐酸维拉帕米,(±)-Verapamil hydrochlorid,Verapamil HCl,Calcan hydrochloride

P450; Calcium Channel; P-gp Membrane transporter/Ion channel; Metabolism; Neuroscience
Verapamil hydrochloride (Verapamil HCl) 是一种钙通道阻滞剂,是一种可口服的 P 糖蛋白 (P-gp) 抑制剂,可抑制CYP3A4,用于高血压、心律不齐和心绞痛的研究。
T2657 Elacridar

GW0918,依克立达,GW120918,GF120918,GG918

BCRP; P-gp Membrane transporter/Ion channel; Neuroscience
Elacridar (GG918) 是一种有效的 P-糖蛋白和BCRP 的抑制剂。
T1222 Trifluoperazine dihydrochloride

Trifluoperazine 2HCl,盐酸三氟拉嗪,SKF5019,Urinox

CaMK; Dopamine Receptor; Influenza Virus; Adrenergic Receptor; P-gp; Autophagy Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
Trifluoperazine dihydrochloride (SKF5019) 是一种抗精神病药物,靶向中枢多巴胺受体。它是流感病毒形态发生的可逆抑制剂,是NUPR1抑制剂,具有抗癌活性。它是钙调蛋白抑制剂,还可抑制 P-糖蛋白,可研究精神分裂症。
T0100 Atazanavir sulfate

阿扎那韦硫酸盐,BMS-232632,BMS-232632 sulfate,硫酸阿扎那韦

P450; SARS-CoV; HIV Protease; P-gp Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
Atazanavir sulfate (BMS-232632 sulfate) 是一种氮杂肽和 HIV 蛋白酶抑制剂,与其他抗 HIV 药物联合用于治疗 HIV 感染和艾滋病。它也是SARS-CoV 3CLpro 抑制剂,IC50为 3.49 μM。
T6018 Zosuquidar trihydrochloride

唑喹达三盐酸盐,Zosuquidar (LY335979) 3HCl,RS 33295-198 trihydrochloride,RS 33295-198 (D06387) 3HCl,Zosuquidar 3HCl,LY-335979 trihydrochloride

P-gp Membrane transporter/Ion channel; Neuroscience
Zosuquidar trihydrochloride (LY-335979 trihydrochloride) 是一种P-糖蛋白抑制剂,Ki 值为 59 nM。
T22680 CP-100356 hydrochloride

CP-100356 HCl,CP 100356 hydrochloride

BCRP Membrane transporter/Ion channel
CP-100356 hydrochloride 是一种具有口服活性和低微摩尔的 MDR1 (P-gp) 和 BCRP 双重抑制剂,是核苷酸衍生的底物类似物,对 MDR1 介导的 Calcein-AM 转运 和 BCRP 介导的 Prazosin 转运有抑制作用。CP-100356 抑制 OATP1B1,可在黑暗中诱导气孔张开。
T67821 GS-9191 PM

BCRP; Antiviral Immunology/Inflammation; Membrane transporter/Ion channel
GS-9191 PM 是一种新型抗瘤病毒化合物,是核苷酸类似物9-(2-膦酰甲氧基乙基)-N6-环丙基-2,6-二氨基嘌呤(cPrPMEDAP)的双酰胺类前药。GS-9191 PM 是MDR1和BCRP的强抑制剂。GS-9191 PM 具有抗增殖活性和抗瘤病毒活性
T4595 YHO-13177

YHO 13177,YHO13177

BCRP Membrane transporter/Ion channel
YHO-13177 是高活性乳腺癌耐药蛋白多药转运通道(BCRP)抑制剂,可增强SN-38活性。
T31069 CP-615003

CP 615003

CP-615003 is a Mdr1 P-glycoprotein substrate.
T28901 T-2007

5,5-Diphenylbarbituric acid,DPB

T-2007 is an α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist and gamma-aminobutyric acid (GABA) receptor agonist. T2007 and its analogs upregulates CYP3A4 and MDR1. T-2007 depressed both the degree and the duration of postt
T71279 BPR1K653

BPR1K653 is a potent Aurora kinase inhibitor with potential anticancder activity. BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent ...
T72921 Reversin 121

Reversin 121为P-糖蛋白(P-glycoprotein) 抑制剂,能增加MDR1的ATP酶活性,可逆转P-糖蛋白介导的多药耐药性,适用于癌症研究。
T68568 Encequidar, HCl

Encequidar, also known as HM-30181, is an oral P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. Encequidar showed the highest potency (IC(50)=0.63nM) among several MDR1 inhibitors, including cycloporin A, XR9576, and GF120918, and effectively blocked transepithelial transport of paclitaxel in MDCK monolayers (IC(50)=35.4nM). Encequidar is currently under clinical trials.
T70695 CP 100356

CP 100356 is a specific inhibitor of MDR1 (P-Gp), the protypical ABC transporter. The compound has low uM to nM potency for inhibiting several MDR-1 substrates (calcein-AM, digoxin) in transfected MDCKII cells.
T69897 MC-70 hydrochloride

MC-70 hydrochloride is a potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μM, 9.3 μM, and 73 μM for Caco-2, MDR1, MRP1, and BCRP inhibition, respectively).
T4047L Bisantrene HCl

CL216942,CL-216942,NSC-337766,CL 216942

Bisantrene (CL-216942; NSC 337766) is a topoisomerase II poison and DNA intercalator. It can be used as a Rac1 inhibitor or model compound to study P-glycoprotein-mediated multi-drug resistance (MDR1). Bisantrene inserts and disrupts the configuration of
T13222 TTT-28

Others Others
TTT-28 is a thiazole-valine peptidomimetic, and is a selective ABCB1 (P-gp/MDR1) inhibitor with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocki
T79353 P-gp/BCRP-IN-2

P-gp/BCRP-IN-2(化合物15)为恶二唑衍生物,作为ABC转运蛋白P-glycoprotein(IC50:1.6 nM)及BCRP(IC50:600 nM)的双重抑制剂。该化合物增强了Doxorubicin针对耐药型人腺癌结肠癌细胞系HT29/DX及MDCK-MDR1细胞的抗增殖效果。
T68656 Brivudine monophosphate

Brivudine monophosphate is a phosphate ester of Brivudine. Brivudine, also known as bromovinyl-deoxyuridine, is a uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. In vitro, bromovinyl-deoxyuridine (BVDU) has been shown to downregulate the multifunctional DNA repair enzyme APEX nuclease 1, resulting in the inhibition of DNA repair and the induction of apoptosis. In addition, this agent may inhibit the expression of STAT3 (signal transducer and activator...
T36807 Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)

Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km= 75 μM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transportviaMRP2 and the transport of other MRP2 ...
T36847 Coelenterazine hcp

Coelenterazine hcp is a synthetic bioluminescent luciferin that displays an emission maximum of 445 nm.1It has been used as a calcium indicator and substrate to quantifyRenillaluciferase activity.1,2,3 1.Sabnis, R.W.Handbook of biological dyes and stains: Synthesis and industrial applications(2010) 2.Shimomura, O., Kishi, Y., and Inouye, S.The relative rate of aequorin regeneration from apoaequorin and coelenterazine analoguesBiochemistry Journal296(Pt 3)549-551(1993) 3.Pichler, A., Prior, J.L.,...

化合物

P-gp inhibitor 1
Cat.No: T12341
Synonym:
Target: Others, P-gp
Dofequidar fumarate
Cat.No: T11071
Synonym: MS-209
Target: P-gp
Polyoxyethylene stearate
Cat.No: T16561
Synonym: POES,聚氧乙烯硬脂酸酯
Target: Antibacterial, P-gp
Encequidar
Cat.No: T8426
Synonym: HM30181,HM30181A
Target: P-gp
Tariquidar
Cat.No: T6287
Synonym: XR9576,他立喹达
Target: P-gp
Selamectin
Cat.No: T4059
Synonym: UK-124114,司拉克丁,塞拉菌素
Target: Chloride channel, P-gp, Parasite
Risperidone
Cat.No: T0351
Synonym: Risperidal,R 64 766,利培酮
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, P-gp
Encequidar mesylate
Cat.No: T11578L
Synonym: HM30181 mesylate,HM30181A mesylate
Target: P-gp
Zamicastat
Cat.No: T13383
Synonym: BIA 5-1058
Target: BCRP, Hydroxylase, P-gp
Trifluoperazine
Cat.No: T8389
Synonym: 三氟拉嗪,trifluoroperazine
Target: CaMK, Dopamine Receptor, Influenza Virus, Adrenergic Receptor, P-gp, Autophagy
Glibenclamide
Cat.No: T1634
Synonym: 格列本脲,Glyburide
Target: Potassium Channel, Mitochondrial Metabolism, CFTR, P-gp, Autophagy
Atazanavir
Cat.No: T0100L
Synonym: Zrivada,Reyataz,Latazanavir,阿扎那韦,BMS-232632
Target: P450, SARS-CoV, HIV Protease, P-gp
Verapamil
Cat.No: T20656
Synonym: NSC 135784,维拉帕米,NSC-135784,CP-16533-1,(±)-Verapamil
Target: P450, Calcium Channel, P-gp
Norverapamil hydrochloride
Cat.No: T16339
Synonym: (±)-Norverapamil hydrochloride,D591 hydrochloride,盐酸去甲维拉帕米
Target: Calcium Channel, P-gp, Drug Metabolite
Verapamil hydrochloride
Cat.No: T1010
Synonym: Manidon,盐酸维拉帕米,(±)-Verapamil hydrochlorid,Verapamil HCl,Calcan hydrochloride
Target: P450, Calcium Channel, P-gp
Elacridar
Cat.No: T2657
Synonym: GW0918,依克立达,GW120918,GF120918,GG918
Target: BCRP, P-gp
Trifluoperazine dihydrochloride
Cat.No: T1222
Synonym: Trifluoperazine 2HCl,盐酸三氟拉嗪,SKF5019,Urinox
Target: CaMK, Dopamine Receptor, Influenza Virus, Adrenergic Receptor, P-gp, Autophagy
Atazanavir sulfate
Cat.No: T0100
Synonym: 阿扎那韦硫酸盐,BMS-232632,BMS-232632 sulfate,硫酸阿扎那韦
Target: P450, SARS-CoV, HIV Protease, P-gp
Zosuquidar trihydrochloride
Cat.No: T6018
Synonym: 唑喹达三盐酸盐,Zosuquidar (LY335979) 3HCl,RS 33295-198 trihydrochloride,RS 33295-198 (D06387) 3HCl,Zosuquidar 3HCl,LY-335979 trihydrochloride
Target: P-gp
CP-100356 hydrochloride
Cat.No: T22680
Synonym: CP-100356 HCl,CP 100356 hydrochloride
Target: BCRP
GS-9191 PM
Cat.No: T67821
Synonym:
Target: BCRP, Antiviral
YHO-13177
Cat.No: T4595
Synonym: YHO 13177,YHO13177
Target: BCRP
CP-615003
Cat.No: T31069
Synonym: CP 615003
Target:
T-2007
Cat.No: T28901
Synonym: 5,5-Diphenylbarbituric acid,DPB
Target:
BPR1K653
Cat.No: T71279
Synonym:
Target:
Reversin 121
Cat.No: T72921
Synonym:
Target:
Encequidar, HCl
Cat.No: T68568
Synonym:
Target:
CP 100356
Cat.No: T70695
Synonym:
Target:
MC-70 hydrochloride
Cat.No: T69897
Synonym:
Target:
Bisantrene HCl
Cat.No: T4047L
Synonym: CL216942,CL-216942,NSC-337766,CL 216942
Target:
TTT-28
Cat.No: T13222
Synonym:
Target: Others
P-gp/BCRP-IN-2
Cat.No: T79353
Synonym:
Target:
Brivudine monophosphate
Cat.No: T68656
Synonym:
Target:
Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)
Cat.No: T36807
Synonym:
Target:
Coelenterazine hcp
Cat.No: T36847
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1651 Furanodiene

Apoptosis; PARP; Reactive Oxygen Species; Caspase; CDK; P-gp Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB; Proteases/Proteasome
Furanodiene 是从姜黄中提取的一种萜类天然产物,可抑制外排转运蛋白Pgp 功能并降低 Pgp 蛋白水平。它通过抗血管生成和诱导ROS 产生,DNA 链断裂和细胞凋亡发挥抗癌作用。
T2S0223 Isosinensetin

异橙黄酮,6-Demethoxynobiletin

Antioxidant; HIV Protease; Antibacterial; P-gp Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; oxidation-reduction; Proteases/Proteasome
Isosinensetin (6-Demethoxynobiletin) 是从青皮中提取的一种甲氧基黄酮,具有抗氧化和抑制 HIV-1 蛋白酶的活性。
T3S0012 coniferyl ferulate

P-gp; GST Membrane transporter/Ion channel; Neuroscience; oxidation-reduction
Coniferyl ferulate 是从川芎中提取的一种天然产物,是强效的谷胱甘肽 S-转移酶抑制剂,强抑制人胎盘型谷胱甘肽 S-转移酶,IC50为 0.3 μM。它还可逆转多药耐药性并下调 P-糖蛋白。
T3002 Piperine

胡椒碱,1-Piperoylpiperidine,Bioperine

P450; Endogenous Metabolite; P-gp; Autophagy Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience
Piperine (Bioperine) 是从胡椒中分离的一种生物碱,可以抑制P-糖蛋白和 CYP3A4 的活性,在HeLa 细胞中的IC50值为61.94±0.054 μg/mL。它已用于研究治疗多发性骨髓瘤和吞咽障碍的试验。
TN4761 Phellamurin

P-gp Membrane transporter/Ion channel; Neuroscience
Phellamurin 是一种来自黄檗叶的黄酮糖苷,可诱导细胞凋亡,具有抗肿瘤活性。它抑制肠道 P-糖蛋白,还抑制凤蝶的产卵。
TJS1159 Chrysosplenetin

猫眼草黄素,Chrysosptertin B

P450; Ferroptosis; P-gp Apoptosis; Membrane transporter/Ion channel; Metabolism; Neuroscience
Chrysosplenetin 是青蒿和其他几种中草药中的一种多甲氧基化黄酮类天然产物,抑制 P-gp 活性并逆转由青蒿素诱导的上调的 P-gp 和 MDR1 水平。
T2S0271 Voacamine

老刺木胺,Voacanginine

Cannabinoid Receptor; P-gp GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
Voacamine (Voacanginine) 是非洲马铃果中的一种吲哚生物碱,可抑制多药耐药肿瘤细胞中的 P-糖蛋白作用,具有强效的大麻素 CB1受体拮抗活性。
T2S1200 Sinapine

Antioxidant; P-gp; AChE Membrane transporter/Ion channel; Neuroscience; oxidation-reduction
Sinapine 是萝卜中分离出来的一种生物碱,具有抗炎、抗氧化、抗肿瘤、抗血管生成和放射防护作用。它还是乙酰胆碱酯酶抑制剂,可用于研究阿尔茨海默症,共济失调,重症肌无力和帕金森氏病。
T4034 Solamargine

Solamargin,δ-Solanigrine,澳洲茄边碱

Apoptosis; p38 MAPK; P-gp; STAT Apoptosis; JAK/STAT signaling; MAPK; Membrane transporter/Ion channel; Neuroscience; Stem Cells
Solamargine (δ-Solanigrine) 是一种来源于茄属植物的类固醇 Solasodine 的衍生物,诱导非选择性细胞毒性和 P-gp 抑制作用。它通过下调 MMP-2 和 MMP-9 的表达和活性来显著抑制 HepG2 细胞的迁移和侵袭,在多种癌症中均表现出抗癌活性。
T3392 Sinapine thiocyanate

P-gp; AChE Membrane transporter/Ion channel; Neuroscience
Sinapine thiocyanate 是萝卜中分离出来的一种生物碱,具有抗炎、抗氧化、抗肿瘤、抗血管生成和放射防护作用。它还是乙酰胆碱酯酶抑制剂,可用于研究阿尔茨海默症,共济失调,重症肌无力和帕金森氏病。
TN1525 Convallatoxin

K-毒毛旋花子配质-3-L-鼠李糖甙,铃兰毒苷

NF-κB; P-gp; PPAR DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB
Convallatoxin 是从铃兰分离得到的一种强心苷。它是 P-糖蛋白底物,并识别 Val982 是参与其转运的重要氨基酸。它是配体诱导的 MOR 胞吞作用的增强剂,通过激活PPARγ和抑制NF-κB 改善结肠炎,具有抗炎和抗增殖特性。
T2799 (20S)-Protopanaxadiol

20-Epiprotopanaxadiol,20(S)-APPD,20 (S)-原人参二醇,原人参二醇

Apoptosis; Reactive Oxygen Species; P-gp Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) 是人参皂甙的代谢产物,是一种凋亡诱导剂,抑制Akt 活性并诱导多种肿瘤细胞凋亡。
TN1757 Hypophyllanthin

叶下珠次素,(7S,8S,9R)-9-(3,4-二甲氧基苯基)-6,7,8,9-四氢-4-甲氧基-7,8-双(甲氧基甲基)萘并[1,2-D]-1,3-二恶茂

Potassium Channel; Calcium Channel; P-gp Membrane transporter/Ion channel; Metabolism; Neuroscience
Hypophyllanthin 是珠子草中的一种木脂素,能直接抑制 P-gp 的活性,具有很强的抗炎活性。
T19768 γ-Tocotrienol

gamma Tocotrienol,gammaTocotrienol,gamma-Tocotrienol,D-gamma-Tocotrienol,Plastochromanol,γ-生育三烯酚

Others Others
γ-Tocotrienol (Plastochromanol) 是一种维生素 E 的活性形式。
TCS2336 Evodine

P-gp Membrane transporter/Ion channel; Neuroscience
Evodine 是吴茱萸中的主要柠檬苦素,是P-gp 有效抑制剂,可通过保留抗氧化剂防御系统,针对谷氨酸诱导的毒性具有保护作用。
T4085 Paris saponin VII

重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII

Apoptosis; BCL; Others; PARP; p38 MAPK; Akt; Caspase; P-gp; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Membrane transporter/Ion channel; Neuroscience; Others; PI3K/Akt/mTOR signaling; Proteases/Proteasome
Paris saponin VII (Dioscini) 是从延龄草的根和根茎中分离的一种甾体皂苷。它减弱线粒体膜电位,增加凋亡相关蛋白的表达,并降低Bcl-2、caspase-9、caspase-3、PARP-1和p-Akt 的蛋白表达水平。它在 K562/ADR 细胞中诱导强烈的自噬,可研究白血病。
T2S0265 Robinin

NSC 9222,刺槐素

TLR Immunology/Inflammation
Flavone glycoside from Robinia with antibacterial and diuretic properties; derived from kaempferol.The ability of robinin to reverse the multidrug resistance of the human colon cancer cell line Colo 320 expreβing MDR1/LRP was explored by monitoring their uptake of Rhodamine 123, but was shown to have minimal effect. Robinin (NSC-9222) was detected in lysates of the human breast cancer cell line MCF-7 using liquid chromatography-tandem maβ spectrometry.
T5813 BYAKANGELICIN

Reductase Endocrinology/Hormones; Metabolism
Byakangelicin 是发现于当归根中的一种活性化合物,可作为调节剂,改善各种活性化合物 (Umb,Cur 和 Dox) 的脑积累,增强研究效果。它提高所有PXR 靶基因 (如MDR1) 的表达,并广泛的诱导药物-药物相互作用。它可抑制性激素的作用,可能会增加内源激素的分解代谢。
TN3937 ent-16alpha,17-Dihydroxyatisan-3-one

P-gp Membrane transporter/Ion channel; Neuroscience
ent-16alpha,17-Dihydroxyatisan-3-one and ent-16alpha,17-dihydroxykauran-3-one have apoptosis induction activities on L5178 human MDR1 gene-transfected mouse lymphoma cells.
T72802 Spongionellol A

Spongionellol A 是一种 MDR1(p-糖蛋白) 抑制剂。Spongionellol A 通过诱导 caspase 依赖性的凋亡 (apoptosis) 而对前列腺癌细胞具有较强的细胞毒活性和选择性。Spongionellol A 可用于癌症的研究,如前列腺癌。

天然产物

Furanodiene
Cat.No: TN1651
Synonym:
Target: Apoptosis, PARP, Reactive Oxygen Species, Caspase, CDK, P-gp
Isosinensetin
Cat.No: T2S0223
Synonym: 异橙黄酮,6-Demethoxynobiletin
Target: Antioxidant, HIV Protease, Antibacterial, P-gp
coniferyl ferulate
Cat.No: T3S0012
Synonym:
Target: P-gp, GST
Piperine
Cat.No: T3002
Synonym: 胡椒碱,1-Piperoylpiperidine,Bioperine
Target: P450, Endogenous Metabolite, P-gp, Autophagy
Phellamurin
Cat.No: TN4761
Synonym:
Target: P-gp
Chrysosplenetin
Cat.No: TJS1159
Synonym: 猫眼草黄素,Chrysosptertin B
Target: P450, Ferroptosis, P-gp
Voacamine
Cat.No: T2S0271
Synonym: 老刺木胺,Voacanginine
Target: Cannabinoid Receptor, P-gp
Sinapine
Cat.No: T2S1200
Synonym:
Target: Antioxidant, P-gp, AChE
Solamargine
Cat.No: T4034
Synonym: Solamargin,δ-Solanigrine,澳洲茄边碱
Target: Apoptosis, p38 MAPK, P-gp, STAT
Sinapine thiocyanate
Cat.No: T3392
Synonym:
Target: P-gp, AChE
Convallatoxin
Cat.No: TN1525
Synonym: K-毒毛旋花子配质-3-L-鼠李糖甙,铃兰毒苷
Target: NF-κB, P-gp, PPAR
(20S)-Protopanaxadiol
Cat.No: T2799
Synonym: 20-Epiprotopanaxadiol,20(S)-APPD,20 (S)-原人参二醇,原人参二醇
Target: Apoptosis, Reactive Oxygen Species, P-gp
Hypophyllanthin
Cat.No: TN1757
Synonym: 叶下珠次素,(7S,8S,9R)-9-(3,4-二甲氧基苯基)-6,7,8,9-四氢-4-甲氧基-7,8-双(甲氧基甲基)萘并[1,2-D]-1,3-二恶茂
Target: Potassium Channel, Calcium Channel, P-gp
γ-Tocotrienol
Cat.No: T19768
Synonym: gamma Tocotrienol,gammaTocotrienol,gamma-Tocotrienol,D-gamma-Tocotrienol,Plastochromanol,γ-生育三烯酚
Target: Others
Evodine
Cat.No: TCS2336
Synonym:
Target: P-gp
Paris saponin VII
Cat.No: T4085
Synonym: 重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII
Target: Apoptosis, BCL, Others, PARP, p38 MAPK, Akt, Caspase, P-gp, Autophagy
Robinin
Cat.No: T2S0265
Synonym: NSC 9222,刺槐素
Target: TLR
BYAKANGELICIN
Cat.No: T5813
Synonym:
Target: Reductase
ent-16alpha,17-Dihydroxyatisan-3-one
Cat.No: TN3937
Synonym:
Target: P-gp
Spongionellol A
Cat.No: T72802
Synonym:
Target:
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