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72

抑制剂 & 化合物

35

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Cat. No. Product Name Target Signaling Pathways
T9982 PU23

MRP Immunology/Inflammation
PU 23 是一种多药抗性蛋白4(MRP4)的抑制剂。
T1248 Sulfanitran

磺胺硝苯,乙酰磺胺对硝基苯

Antibacterial; Autophagy Autophagy; Microbiology/Virology
Sulfanitran 是一种用于家禽业的磺胺类抗生素。它也是一种多药耐药蛋白 2 (MRP2) 激动剂,可增加 MRP2 对雌二醇 17-β-D-葡糖醛酸的亲和力。
T8596 Ceefourin 1

MRP Immunology/Inflammation
Ceefourin 1 是一种具有高度选择性的多药抗性蛋白 4 (MRP4) 抑制剂。它能够抑制多种 MRP4 底物的转运,但对其他 ABC 转运蛋白无影响。它是苯并噻唑,常作为高危神经母细胞瘤的化学增敏剂。
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。
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。
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)。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
T9944 3-(9-Chloro-3-methyl-4-oxoisoxazolo[4,3-c]quinolin-5(4H)-yl)-N-(3,4,5-trimethoxyphenyl)benzeneacetamide

MRP Immunology/Inflammation
3-(9-Chloro-3-methyl-4-oxoisoxazolo[4,3-c]quinolin-5(4H)-yl)-N-(3,4,5-trimethoxyphenyl)benzeneacetamide inhibits multidrug resistance protein (MRP1).
T27954 LY-402913

LY 402913,LY402913

MRP Immunology/Inflammation
LY-402913 是一种选择性多药耐药蛋白 (MRP1) 抑制剂。
T68163 timcodar

Timcodar 也被称为VX-853,是一种多药耐药性抑制剂。
T3581 KS176

Potassium Channel; BCRP Membrane transporter/Ion channel
KS176是选择性高活性乳腺癌耐药蛋白多药转运通道抑制剂,在Pheo A 和Hoechst 检测中,IC50值分别为0.59和1.39 μM。
T60009 YS-370

P-gp Membrane transporter/Ion channel; Neuroscience
YS-370 是一种具有口服活性的 P-gp 抑制剂,对 CYP3A4 有中度抑制作用。 YS-370 有效逆转对紫杉醇和秋水仙碱的多药耐药性,与紫杉醇联合应用表现出更强的抗肿瘤活性。
T5699 SSE15206

Apoptosis; Microtubule Associated Apoptosis; Cytoskeletal Signaling
SSE15206 是一种克服多药耐药性的微管聚合抑制剂,其在 HCT116 细胞中的 GI50值为 197 nM。由于癌细胞中纺锤体形成不完整,导致 G2/M 停滞,有丝分裂异常。
T64133L Laniquidar TFA

Laniquidar TFA(197509-46-9 Free base),R101933

P-gp Membrane transporter/Ion channel; Neuroscience
Laniquidar TFA (R101933) 是一种新型口服非竞争性P-糖蛋白(P-gp)抑制剂,IC50 值为 0.51 μM。Laniquidar的生物利用度有限,可用于调节多药耐药性转运体。Laniquidar可用于研究急性髓性白血病(AML)和骨髓增生异常综合征(MDS)。
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。
T24785 S-Fcme

S Fcme,SFcme

S-Fcme is an activator of multidrug resistance transporter that acts by stimulating the multidrug resistance transporter ATPase activity and competing for drug binding.
T26417 A 39355

A39355,A-39355

A 39355 may specifically overcome multidrug resistance without the serious hypotensive effects associated with calcium antagonists.
T70683 NA 382

NA 382 is a staurosporine derivative that inhibits multidrug resistance.
T23868 Ceefourin-2

Ceefourin2,Ceefourin 2

Ceefourin-2 is a highly selective multidrug resistance protein 4 inhibitor.
T12714 Reversan

CBLC4H10

Others Others
Reversan is a potent and nontoxic multidrug inhibitor of resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp).
T27946 LY-329146

LY 329146

LY-329146 is a selective estrogen receptor modulator (SERM). LY-329146 prevents doxorubicin resistance in tumor cells expressing multidrug resistance-associated protein (MRP) by inhibiting the binding of MRP substrates to the estrogen receptor.
T24005 DJ101

DJ-101,DJ 101

DJ101is an effective and metabolically stable inhibitor of tubulin. It can circumvent the drug efflux pumps responsible for multidrug resistance of existing tubulin inhibitors.
T28173 NIK-250

NIK250

NIK-250 is a P-glycoprotein inhibitor. NIK250 could reverse multidrug resistance in human glioma cells.
T26180 Sdz 280 446

Sdz 280,446,Sdz 280-446

Sdz 280 446 is one of the most active cyclopeptolide of many resistance-modifying agents in restoring rhodamine-123 retention within multidrug-resistant P388 cells.
T71582 Niguldipine Free Base

Niguldipine Free Base is a calcium channel blocker and a₁-adrenergic receptor antagonist and a clinical modulator of multidrug resistance.
T29169 XR9051 Hydrochloride

XR9051 Hydrochloride, a potent modulator of P-glycoprotein-mediated multidrug resistance (MDR), inhibits the binding of cytotoxics to P-glycoprotein.
T26413 A 30312

A-30312,A30312

A 30312 is a fused indole, which overcomes multidrug resistance in P388/Adr cells in vitro. It potentiates the cytotoxicity of the antitumor drugs Adriamycin, vincristine and vinblastine in multidrug-resistant cells with no effect on drug-sensitive parent P388 cells.
T26229 ST7710AA1

ST-7710-AA1,ST 7710 AA1

ST7710AA1 is a PARP-1 inhibitor that acts by showing significant in vitro target inhibition and capability to substantially bypass the multidrug resistance mediated by Pgp.
T15384 Glesatinib

MGCD265

c-Met/HGFR Tyrosine Kinase/Adaptors
Glesatinib is an orally active and potent dual inhibitor of MET/SMO. Glesatinib is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.
T6287L Tariquidar dimesylate

D 06008,XR9576,D06008,XR 9576,Tariquidar dimesilate,XR-9576

Tariquidar is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs.
T15383 Glesatinib hydrochloride

MGCD265 hydrochloride

c-Met/HGFR Tyrosine Kinase/Adaptors
Glesatinib hydrochloride is an orally active and potent dual inhibitor of MET/SMO. Glesatinib hydrochloride is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.
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
T68209 Kopsoffinol

Kopsoffinol is a bisindole alkaloid that has been shown to have in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells.
T74826 AcrB-IN-1

AcrB-IN-1 (Compound H6) 是一种有效的 AcrB 抑制剂。AcrB-IN-1 可用于逆转细菌多药耐药。
T68326 Annamycin

Annamycin is a semi-synthetic doxorubicin analogue annamycin with antineoplastic activity. Annamycin intercalates into DNA and inhibits topoisomerase II, resulting in the inhibition of DNA replication and repair and RNA and protein synthesis. This agent circumvents multidrug-resistance (MDR) transporters, including P-glycoprotein (P-gp).

化合物

PU23
Cat.No: T9982
Synonym:
Target: MRP
Sulfanitran
Cat.No: T1248
Synonym: 磺胺硝苯,乙酰磺胺对硝基苯
Target: Antibacterial, Autophagy
Ceefourin 1
Cat.No: T8596
Synonym:
Target: MRP
Zamicastat
Cat.No: T13383
Synonym: BIA 5-1058
Target: BCRP, Hydroxylase, P-gp
Polyoxyethylene stearate
Cat.No: T16561
Synonym: POES,聚氧乙烯硬脂酸酯
Target: Antibacterial, P-gp
P-gp inhibitor 1
Cat.No: T12341
Synonym:
Target: Others, P-gp
Encequidar
Cat.No: T8426
Synonym: HM30181,HM30181A
Target: P-gp
Dofequidar fumarate
Cat.No: T11071
Synonym: MS-209
Target: P-gp
Tariquidar
Cat.No: T6287
Synonym: XR9576,他立喹达
Target: P-gp
Risperidone
Cat.No: T0351
Synonym: Risperidal,R 64 766,利培酮
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, P-gp
Selamectin
Cat.No: T4059
Synonym: UK-124114,司拉克丁,塞拉菌素
Target: Chloride channel, P-gp, Parasite
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
Encequidar mesylate
Cat.No: T11578L
Synonym: HM30181 mesylate,HM30181A mesylate
Target: P-gp
Elacridar
Cat.No: T2657
Synonym: GW0918,依克立达,GW120918,GF120918,GG918
Target: BCRP, P-gp
Atazanavir
Cat.No: T0100L
Synonym: Zrivada,Reyataz,Latazanavir,阿扎那韦,BMS-232632
Target: P450, SARS-CoV, HIV Protease, 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
Verapamil
Cat.No: T20656
Synonym: NSC 135784,维拉帕米,NSC-135784,CP-16533-1,(±)-Verapamil
Target: P450, Calcium Channel, 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
3-(9-Chloro-3-methyl-4-oxoisoxazolo[4,3-c]quinolin-5(4H)-yl)-N-(3,4,5-trimethoxyphenyl)benzeneacetamide
Cat.No: T9944
Synonym:
Target: MRP
LY-402913
Cat.No: T27954
Synonym: LY 402913,LY402913
Target: MRP
timcodar
Cat.No: T68163
Synonym:
Target:
KS176
Cat.No: T3581
Synonym:
Target: Potassium Channel, BCRP
YS-370
Cat.No: T60009
Synonym:
Target: P-gp
SSE15206
Cat.No: T5699
Synonym:
Target: Apoptosis, Microtubule Associated
Laniquidar TFA
Cat.No: T64133L
Synonym: Laniquidar TFA(197509-46-9 Free base),R101933
Target: P-gp
MK-571 sodium
Cat.No: T3148
Synonym: L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid
Target: Leukotriene Receptor, LTR
S-Fcme
Cat.No: T24785
Synonym: S Fcme,SFcme
Target:
A 39355
Cat.No: T26417
Synonym: A39355,A-39355
Target:
NA 382
Cat.No: T70683
Synonym:
Target:
Ceefourin-2
Cat.No: T23868
Synonym: Ceefourin2,Ceefourin 2
Target:
Reversan
Cat.No: T12714
Synonym: CBLC4H10
Target: Others
LY-329146
Cat.No: T27946
Synonym: LY 329146
Target:
DJ101
Cat.No: T24005
Synonym: DJ-101,DJ 101
Target:
NIK-250
Cat.No: T28173
Synonym: NIK250
Target:
Sdz 280 446
Cat.No: T26180
Synonym: Sdz 280,446,Sdz 280-446
Target:
Niguldipine Free Base
Cat.No: T71582
Synonym:
Target:
XR9051 Hydrochloride
Cat.No: T29169
Synonym:
Target:
A 30312
Cat.No: T26413
Synonym: A-30312,A30312
Target:
ST7710AA1
Cat.No: T26229
Synonym: ST-7710-AA1,ST 7710 AA1
Target:
Glesatinib
Cat.No: T15384
Synonym: MGCD265
Target: c-Met/HGFR
Tariquidar dimesylate
Cat.No: T6287L
Synonym: D 06008,XR9576,D06008,XR 9576,Tariquidar dimesilate,XR-9576
Target:
Glesatinib hydrochloride
Cat.No: T15383
Synonym: MGCD265 hydrochloride
Target: c-Met/HGFR
TTT-28
Cat.No: T13222
Synonym:
Target: Others
Kopsoffinol
Cat.No: T68209
Synonym:
Target:
AcrB-IN-1
Cat.No: T74826
Synonym:
Target:
Annamycin
Cat.No: T68326
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
T3S2019 Lathyrol

Others Others
Lathyrol 是一种具有抗癌功能的天然产物。
T6S1842 Tenacissoside G

Tenacissimoside A,通关藤苷G

Others Others
Tenacissoside G 是一种 C21 甾体,来自于Marsdenia tenacissima 茎部。它可逆转 P-糖蛋白过度表达的多药耐药癌细胞的多药耐药。
T6S0095 Genkwanin

7-O-Methylapigenin,Puddumetin,Apigenin 7-methyl ether,芫花素

Virus Protease Microbiology/Virology
Genkwanin (Apigenin 7-methyl ether) 是一种O-甲基化黄酮,有抗炎活性,通过被动扩散和多药耐药蛋白介导的外排机制转运。
TN2256 Taccalonolide B

根薯酮内酯B,根薯酮内酯 B

Microtubule Associated Cytoskeletal Signaling
Taccalonolide B 是从广西裂果薯中分离得到的一种微管稳定剂,具有抗肿瘤活性。它抑制 SK-OV-3 细胞的生长,IC50 为 208 nM,在体外对过表达 P-糖蛋白 (Pgp) 和多药耐药蛋白 (MRP7) 的细胞系有效。
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.
T4A2399 Cinobufotalin

华蟾毒它灵,华蟾素

IL Receptor; Akt; MRP; P-gp Cytoskeletal Signaling; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; PI3K/Akt/mTOR signaling
Cinobufotalin 是一种从蟾蜍的皮肤分泌物中提取的强心类固醇或丁二烯内酯。它已被用作强心药,利尿药和止血药,也是潜在的抗肺癌药物。
TN2254 Taccalonolide A

根薯酮内酯A,根薯酮内酯 A

Apoptosis; Microtubule Associated Apoptosis; Cytoskeletal Signaling
Taccalonolide A 是从水田七根茎中分离得到的一种类固醇,具有细胞毒性和抗疟活性。它在体外对过表达 p 糖蛋白、多药耐药蛋白 7 细胞系有抑制作用,抑制 SK-OV-3 细胞生长的 IC50值为 622 nM。它是微管稳定剂,能引起 G2-M 期滞留、Bcl-2 磷酸化,并引发细胞凋亡。
T4S1419 (±)-Praeruptorin A

Praeruptorin A,(±)-白花前胡甲素,白花前胡甲素,(-)-Praeruptorin A

p38 MAPK; Calcium Channel; Akt Cytoskeletal Signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling
(±)-Praeruptorin A 是来自白花前胡的干燥根中的一种主要成分,用于研究伴有厚痰和呼吸困难的咳嗽,非天生性咳嗽和上呼吸道感染。它是顺式-内酯 (CKL) 的二酯化产物,可作为 Ca2+-反流阻滞剂,用于高血压的研究。
T13956 Uvarigrin

Others Others
Uvarigrin induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation. Uvarigrin is isolated from the roots of Uvaria calamistrata.
T3S2016 Epoxylathyrol

Others Others
Epoxylathyrol derivatives have modulation of ABCB1-mediated multidrug resistance in human colon adenocarcinoma and mouse T-Lymphoma cells.
TMA0017 Sideroxylin

Antifection Microbiology/Virology
Sideroxylin can synergistically enhance the antimicrobial activity of the alkaloid berberine (also a constituent of H. canadensis) against Staphylococcus aureus by inhibition of the NorA multidrug resistance pump.
TN4962 Scholaricine

Others Others
Scholaricine reverses multidrug resistance in vincristine-resistant KB cells.
TN3077 5,5'-Dimethoxylariciresinol 4-O-glucoside

5,5'-二甲氧基落叶松脂素4-O-葡萄糖苷

Others Others
5,5'-Dimethoxylariciresinol-4'-O-beta-D-glucoside is shown to effectively enhance chemosensitivity of resistant cells, which makes it may be a suitable candidate for potential multidrug resistance (MDR)-reversing agents.
T23610 Acerinol

Acerinol is an active ingredient from traditional Chinese medicinal herbs. It could be used as a cancer multidrug resistance reversal agent. Acerinol can significantly stimulate the activity of ABCB1 ATPase without affecting the expression of ABCB1 on nei
T83055 Anti-inflammatory agent 57

Anti-inflammatory agent 57(Compound 13),一种天然产自Peucedanum praeruptorum根部的吡喃香豆素,既能逆转多药耐药性(MDR)又具备抗炎效果。
T72737 Ganoderic acid R

Ganoderic acid R为一种高效的抗癌化合物,通过促进肿瘤细胞系的凋亡(apoptosis)机制来抑制其生长。它对多药耐药(MDR)肿瘤细胞系(KB-A-1/Dox)及敏感肿瘤细胞系(KB-A-1)展现出显著的细胞毒性效应。
T15097 Deoxynivalenol

Vomitoxin,4-Deoxynivalenol

Deoxynivalenol (Vomitoxin) 是一种单端孢菌素家族镰刀菌属产生的霉菌毒素,常见于受到污染的食物和饲料中。Deoxynivalenol 通过紧密连接处的细胞旁路来穿过肠粘膜。Deoxynivalenol 转运不受P-糖蛋白 (PgP) 或多药耐药相关蛋白 (MRP) 抑制剂的影响。Deoxynivalenol 通常会导致人类和动物腹泻、呕吐和胃肠道炎症。
TN5414 Wallichinine

Wallichinine shows inhibitory activity on platelet aggregation caused by platelet activating factor (PAF). Wallichinine with ABCB1 presents valuable clues for the development of novel MDR reversal reagents from natural products, wallichinine can significa
TN5153 Torilin

MMP; ERK; IκB/IKK; p38 MAPK; NF-κB; Tyrosinase; Reductase; DNA/RNA Synthesis; JNK Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Endocrinology/Hormones; MAPK; Metabolism; NF-κB; Proteases/Proteasome
Torilin 是一种睾酮5α还原酶抑制剂,它(IC50=31.7+/-4.23μM)对5α还原酶的抑制作用强于α-亚麻酸(IC50=160.3+/-24.62μM),但弱于非那雄胺(IC50=0.38+/-0.06μM)。Torilin 具有免疫调节、肝脏保护和抗炎特性,它通过限制 TAK1介导的 MAP 激酶和 NF-βB 活化来抑制炎症,它可以减轻关节炎的严重程度,改变 dLN 或关节中的白细胞活化,并恢复血清和脾细胞细胞因子失衡。托利林抑制α-黑素细胞刺激激素激活的 B16黑色素瘤细胞中的黑色素生成,IC(50)值为25μM。Torilin 对枯草芽孢杆菌 ATCC 6633孢子和营养细胞表现出优异的抗菌活性。Torilin 在体内和体外都具有强大的抗血管生成活性,它可能通过抑制肿瘤侵袭来抑制肿瘤发生,逆转癌细胞的多药耐药性,它可以增强阿霉素、长春碱、紫杉醇和秋水仙碱对多药耐药 KB-V1和 MCF7/ADR 细胞的细胞毒性。

天然产物

coniferyl ferulate
Cat.No: T3S0012
Synonym:
Target: P-gp, GST
Phellamurin
Cat.No: TN4761
Synonym:
Target: P-gp
Isosinensetin
Cat.No: T2S0223
Synonym: 异橙黄酮,6-Demethoxynobiletin
Target: Antioxidant, HIV Protease, Antibacterial, P-gp
Voacamine
Cat.No: T2S0271
Synonym: 老刺木胺,Voacanginine
Target: Cannabinoid Receptor, P-gp
Piperine
Cat.No: T3002
Synonym: 胡椒碱,1-Piperoylpiperidine,Bioperine
Target: P450, Endogenous Metabolite, P-gp, Autophagy
Chrysosplenetin
Cat.No: TJS1159
Synonym: 猫眼草黄素,Chrysosptertin B
Target: P450, Ferroptosis, P-gp
Sinapine
Cat.No: T2S1200
Synonym:
Target: Antioxidant, P-gp, AChE
Sinapine thiocyanate
Cat.No: T3392
Synonym:
Target: P-gp, AChE
Solamargine
Cat.No: T4034
Synonym: Solamargin,δ-Solanigrine,澳洲茄边碱
Target: Apoptosis, p38 MAPK, P-gp, STAT
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
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
Evodine
Cat.No: TCS2336
Synonym:
Target: 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
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
Furanodiene
Cat.No: TN1651
Synonym:
Target: Apoptosis, PARP, Reactive Oxygen Species, Caspase, CDK, P-gp
Lathyrol
Cat.No: T3S2019
Synonym:
Target: Others
Tenacissoside G
Cat.No: T6S1842
Synonym: Tenacissimoside A,通关藤苷G
Target: Others
Genkwanin
Cat.No: T6S0095
Synonym: 7-O-Methylapigenin,Puddumetin,Apigenin 7-methyl ether,芫花素
Target: Virus Protease
Taccalonolide B
Cat.No: TN2256
Synonym: 根薯酮内酯B,根薯酮内酯 B
Target: Microtubule Associated
Robinin
Cat.No: T2S0265
Synonym: NSC 9222,刺槐素
Target: TLR
Cinobufotalin
Cat.No: T4A2399
Synonym: 华蟾毒它灵,华蟾素
Target: IL Receptor, Akt, MRP, P-gp
Taccalonolide A
Cat.No: TN2254
Synonym: 根薯酮内酯A,根薯酮内酯 A
Target: Apoptosis, Microtubule Associated
(±)-Praeruptorin A
Cat.No: T4S1419
Synonym: Praeruptorin A,(±)-白花前胡甲素,白花前胡甲素,(-)-Praeruptorin A
Target: p38 MAPK, Calcium Channel, Akt
Uvarigrin
Cat.No: T13956
Synonym:
Target: Others
Epoxylathyrol
Cat.No: T3S2016
Synonym:
Target: Others
Sideroxylin
Cat.No: TMA0017
Synonym:
Target: Antifection
Scholaricine
Cat.No: TN4962
Synonym:
Target: Others
5,5'-Dimethoxylariciresinol 4-O-glucoside
Cat.No: TN3077
Synonym: 5,5'-二甲氧基落叶松脂素4-O-葡萄糖苷
Target: Others
Acerinol
Cat.No: T23610
Synonym:
Target:
Anti-inflammatory agent 57
Cat.No: T83055
Synonym:
Target:
Ganoderic acid R
Cat.No: T72737
Synonym:
Target:
Deoxynivalenol
Cat.No: T15097
Synonym: Vomitoxin,4-Deoxynivalenol
Target:
Wallichinine
Cat.No: TN5414
Synonym:
Target:
Torilin
Cat.No: TN5153
Synonym:
Target: MMP, ERK, IκB/IKK, p38 MAPK, NF-κB, Tyrosinase, Reductase, DNA/RNA Synthesis, JNK
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