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28

抑制剂 & 化合物

3

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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

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

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。

化合物

33-BCRP Inhibitor
Cat.No: T83892
Synonym: 33-Breast Cancer Resistance Protein Inhibitor
Target:
Ko 143
Cat.No: TQ0186
Synonym:
Target: BCRP, ABC
P-gp/BCRP-IN-1
Cat.No: T63267
Synonym:
Target:
P-gp/BCRP-IN-2
Cat.No: T79353
Synonym:
Target:
YHO-13177
Cat.No: T4595
Synonym: YHO 13177,YHO13177
Target: BCRP
KS176
Cat.No: T3581
Synonym:
Target: Potassium Channel, BCRP
Triclabendazole sulfoxide
Cat.No: T38400
Synonym: TCBZ-SO,三氯苯达唑亚砜
Target: BCRP, Parasite
Ceefourin 1
Cat.No: T8596
Synonym:
Target: MRP
PCI 29732
Cat.No: T4337
Synonym: PCI29732,PCI-29732
Target: Others, BCRP, BTK
Zamicastat
Cat.No: T13383
Synonym: BIA 5-1058
Target: BCRP, Hydroxylase, P-gp
Elacridar
Cat.No: T2657
Synonym: GW0918,依克立达,GW120918,GF120918,GG918
Target: BCRP, P-gp
CP-100356 hydrochloride
Cat.No: T22680
Synonym: CP-100356 HCl,CP 100356 hydrochloride
Target: BCRP
YHO-13351 free base
Cat.No: T13365
Synonym:
Target: BCRP
PF-06273340
Cat.No: T19649
Synonym: PF 6273340,PF 06273340,PF6273340,PF-6273340
Target: Trk receptor
GS-9191 PM
Cat.No: T67821
Synonym:
Target: BCRP, Antiviral
(S)-ML753286
Cat.No: T10490
Synonym:
Target: Others
FD 12-9
Cat.No: T11268
Synonym: Ac12Az9
Target: Others
ML753286
Cat.No: T16113
Synonym:
Target: AMPK
Ac32Az19
Cat.No: T73356
Synonym:
Target:
MC-70 hydrochloride
Cat.No: T69897
Synonym:
Target:
YHO-13351
Cat.No: T13366
Synonym:
Target: Epigenetic Reader Domain
UR-MB108
Cat.No: T73369
Synonym:
Target:
Efflux inhibitor-1
Cat.No: T72521
Synonym:
Target:
Atiratecan
Cat.No: T14340
Synonym: TP300
Target: Others
Cefditoren sodium
Cat.No: T1405L
Synonym: Cefditoren pivoxil,Cefditoren,ME-1206,ME1206,ME 1206
Target:
(6R)-ML753286
Cat.No: T72861
Synonym:
Target:
CH-0793076
Cat.No: T14945
Synonym: TP3076
Target: Topoisomerase
CH-0793076 TFA
Cat.No: T73672
Synonym:
Target:
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。

天然产物

5,7-DIMETHOXYFLAVONE
Cat.No: T5778
Synonym:
Target: Anti-infection, P450
Fumitremorgin C
Cat.No: T15355
Synonym: 烟曲霉毒素c,12α-Fumitremorgin C
Target: BCRP, Antibacterial, Antibiotic, ABC
6,8-Diprenylnaringenin
Cat.No: TN3150
Synonym: 6,8-二异戊二烯基柚皮素,Senegalensin,Lonchocarpol A
Target: BCRP, ABC
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