17
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0186 |
Ko 143
|
BCRP; ABC | Membrane transporter/Ion channel |
Ko 143 有效且选择性抑制 ATP 结合盒亚家族 G 成员 2 (ABCG2/BCRP) | |||
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。 | |||
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。 | |||
T38400 |
Triclabendazole sulfoxide
TCBZ-SO,三氯苯达唑亚砜 |
BCRP; Parasite | Membrane transporter/Ion channel; Microbiology/Virology |
Triclabendazole sulfoxide (TCBZ-SO) 是 Triclabendazole 的主要血浆代谢产物。Triclabendazole sulfoxide 具有抗寄生虫活性。Triclabendazole sulfoxide 可以抑制膜转运蛋白ABCG2/BCRP 的活性。 | |||
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。 | |||
T4337 |
PCI 29732
PCI29732,PCI-29732 |
Others; BCRP; BTK | Angiogenesis; Membrane transporter/Ion channel; Others; Tyrosine Kinase/Adaptors |
PCI 29732 是一种有效的可逆BTK 抑制剂,对 BTK、Lck 和 Lyn 的Kiapp 值分别为 8.2、4.6 和 2.5 nM。它通过竞争性结合ABCG2 的 ATP 结合位点来抑制ABCG2的功能。 | |||
T83892 |
33-BCRP Inhibitor
33-Breast Cancer Resistance Protein Inhibitor |
||
33-BCRP抑制剂是一种乳腺癌耐药蛋白(BCRP)的抑制剂。它使得对米托蒽醌耐药的H460/MX20肺癌细胞对米托蒽醌诱导的细胞死亡更加敏感,无论是单独使用还是与UV辐射联合使用。33-BCRP抑制剂还能够增强表达P-糖蛋白(P-gp,亦称为多药耐药蛋白MDR)的KB-C2表皮癌细胞对秋水仙碱诱导的细胞死亡的敏感性。当使用5 µM浓度时,它能增加米托蒽醌在H460/MX20细胞中的细胞内积累。 | |||
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。 | |||
T6200 |
Ledipasvir
GS-5885,雷迪帕韦 |
HCV Protease; SARS-CoV | Microbiology/Virology; Proteases/Proteasome |
Ledipasvir (GS-5885) 是一种丙型肝炎病毒 NS5A 抑制剂。它也是 P-糖蛋白抑制剂和乳腺癌抗性蛋白抑制剂。 | |||
T10490 |
(S)-ML753286
|
Others | Others |
(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor (IC50: 0.6 μM on BCRP efflux transporter). | |||
T37685 |
CAY10719
CAY10719 |
||
CAY10719 is a selective inhibitor of the breast cancer resistance protein ABCG2 (IC50 = 0.23 μM) with little activity at ABCG1. It has been shown to reverse the ABCG2-mediated resistance toward SN 38 and to inhibit ATPase activity. | |||
T14340 |
Atiratecan
TP300 |
Others | Others |
Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. Atiratecan does not inhibit acetylch | |||
T14945 |
CH-0793076
TP3076 |
Topoisomerase | DNA Damage/DNA Repair |
CH-0793076, a hexacyclic camptothecin analog, is an active drug and major metabolite of TP300. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein). CH-0793076 inhibits DNA topoisomerase I (IC50: 2.3 μM). | |||
T73356 | Ac32Az19 | ||
Ac32Az19 是一种有效、无毒、高选择性的 BCRP 抑制剂,在BCRP 过度表达的HEK293/R2细胞中,EC50值为13 nM。 | |||
T73672 | CH-0793076 TFA | ||
CH-0793076 (TP3076) TFA,喜树碱的六环类似物,是 TP300 的活性药物和主要代谢物。CH-0793076 TFA 抑制 DNA 拓扑异构酶 I (DNAtopoisomeraseI),IC50为 2.3 μM。CH-0793076 TFA 对表达 BCRP(乳腺癌耐药蛋白) 的细胞也有活性。 | |||
T72861 | (6R)-ML753286 | ||
(6R)-ML753286 是 ML753286 的异构体。ML753286 是一种口服活性和选择性 BCRP(抗乳腺癌蛋白) 抑制剂,IC50为 0.6 μM。 ML753286 在啮齿动物和人类肝脏 S9 组分中具有高渗透性和低至中等清除率,并且在不同物种中都具有血浆稳定性。 | |||
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 ... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN3150 |
6,8-Diprenylnaringenin
6,8-二异戊二烯基柚皮素,Senegalensin,Lonchocarpol A |
BCRP; ABC | Membrane transporter/Ion channel |
6,8-Diprenylnaringenin (Senegalensin) 是来自蛇麻草 Humulus lupulus 的天然产物。 6,8-Diprenylnaringenin 是一种乳腺癌耐药蛋白 (BCRP) 抑制剂,具有一定雌激素作用。 | |||
T15355 |
Fumitremorgin C
烟曲霉毒素c,12α-Fumitremorgin C |
BCRP; Antibacterial; Antibiotic; ABC | Membrane transporter/Ion channel; Microbiology/Virology |
Fumitremorgin C (12α-Fumitremorgin C) 是ABCG2/BRCP 的选择性抑制剂。 | |||
T3208 |
Brevianamide F
Cyclo-L-tryptophyl-L-proline,cyclo-(L-Trp-L-Pro),Cyclo(L-Pro-L-Trp) |
BCRP; PI3K; Antibacterial | Membrane transporter/Ion channel; Microbiology/Virology; PI3K/Akt/mTOR signaling |
Brevianamide F (Cyclo(L-Pro-L-Trp)) 是一种从Colletotrichum gloeosporioides 中分离得到的真菌毒素,属于天然存在的 2,5-二酮哌嗪类,具有抗菌活性。它具有PI3Kα抑制活性,IC50值为 4.8 µM。 | |||
TN5190 | Tryprostatin A | Topoisomerase; Antifection | DNA Damage/DNA Repair; Microbiology/Virology |
Tryprostatin A is an inhibitor of breast cancer resistance protein. Tryprostatin A and tryprostatin B are indole alkaloid-based fungal products that inhibit mammalian cell cycle at the G2/M phase. |