72
35
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). |
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
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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
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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
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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 |
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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
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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
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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。 |