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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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) | |||
T63267 |
P-gp/BCRP-IN-1
|
||
P-gp/BCRP-IN-1 (compound 19) 是一种潜在的、相对安全的、口服有效的外排转运蛋白(P-gp 和 BCRP) 抑制剂。P-gp/BCRP-IN-1 通过抑制 P-gp 和BCRP 的外排功能产生耐药性逆转,P-gp/BCRP-IN-1可克服紫杉醇的耐药性,提高紫杉醇的口服生物利用度。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T13365 |
YHO-13351 free base
|
BCRP | Membrane transporter/Ion channel |
YHO-13351 free base 是 YHO-13177 的水溶性前药,YHO-13177 是 BCRP 的抑制剂。 | |||
T19649 |
PF-06273340
PF 6273340,PF 06273340,PF6273340,PF-6273340 |
Trk receptor | Tyrosine Kinase/Adaptors |
PF-06273340 是一种口服具有活力的、具有选择性的外周限制性Trk 泛抑制剂。 | |||
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 | |||
T10490 |
(S)-ML753286
|
Others | Others |
(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor (IC50: 0.6 μM on BCRP efflux transporter). | |||
T11268 |
FD 12-9
Ac12Az9 |
Others | Others |
FD 12-9, Anti-glioblastoma activity. is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. | |||
T16113 | ML753286 | AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species. | |||
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。 | |||
T69897 |
MC-70 hydrochloride
|
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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). | |||
T13366 |
YHO-13351
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific BCRP inhibitor. | |||
T73369 |
UR-MB108
|
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UR-MB108 是一种有效的、选择性的ABCG2 (BCRP)抑制剂,IC50值为 79 nM。UR-MB108 在血浆中很稳定。 | |||
T72521 | Efflux inhibitor-1 | ||
Efflux inhibitor-1为一种吡唑啉[1,5-a]嘧啶类外排抑制剂,具有对ABCG2/BCRP和ABCB1的选择性靶向性,优先靶向ABCG2,其IC50值分别为0.45 μM与2.17 μM。 | |||
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 | |||
T1405L |
Cefditoren sodium
Cefditoren pivoxil,Cefditoren,ME-1206,ME1206,ME 1206 |
||
Cefditoren sodium is a cephalosporin antibiotic potentially for the treatment of bacterial infection. The expression levels of Mrp2, Bcrp, Oat2 mRNA were markedly increased, while P-gp and Oct1 mRNA were decreased. In concordance with RT-PCR results, Mrp2 | |||
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。 | |||
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). | |||
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5778 |
5,7-DIMETHOXYFLAVONE
|
Anti-infection; P450 | Metabolism; Microbiology/Virology |
5,7-Dimethoxyflavone 是一种 Kaempferia parviflora 的主要成分,具有抗肿瘤、抗肥胖及抗炎活性。它对细胞色素 P450 (CYP) 3As 具有抑制作用,也是抗乳腺癌蛋白 (BCRP) 抑制剂。 | |||
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。 | |||
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。 |