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T79513 |
ABCG2-IN-1
|
|
BCRP
|
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ABCG2-IN-1 (compound K2), an analog of Ko143, constitutes an orally active inhibitor targeting ABCG2 with an inhibitory concentration (IC50) of 0.13 μM. Demonstrating favorable oral pharmacokinetics in mice, ABCG2-IN-1 s... |
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T79514 |
ABCG2-IN-2
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|
BCRP
|
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ABCG2-IN-2 is a potent inhibitor of ABCG2, exhibiting favorable oral pharmacokinetic profiles in mice, and is applicable for investigating tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) [1]. |
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TQ0186 |
Ko 143
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|
BCRP
,
ABC
|
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Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP). |
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T3581 |
KS176
|
|
Potassium Channel
,
BCRP
|
|
KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter, showing no inhibitory activity against P-gp or MRP1. |
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T4595 |
YHO-13177
|
YHO 13177,YHO13177 |
BCRP
|
|
YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells. |
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T38400 |
Triclabendazole sulfoxide
|
TCBZ-SO |
BCRP
,
Parasite
|
|
Triclabendazole sulfoxide (TCBZ-SO) is a main plasma metabolite of Triclabendazole. Triclabendazole sulfoxide inhibits membrane transporter ABCG2/BCRP and exhibits anti-parasite effects. |
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T8596 |
Ceefourin 1
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|
MRP
|
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Ceefourin 1 is a highly selective multidrug resistance protein 4 (MRP4) inhibitor. |
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T4337 |
PCI 29732
|
PCI29732,PCI-29732 |
Others
,
BCRP
,
BTK
|
|
PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay. |
|
T13383 |
Zamicastat
|
BIA 5-1058 |
BCRP
,
Hydroxylase
,
P-gp
|
|
Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH), and is also a concentration-dependent dual inhibitor of P-gp and BCRP(IC50 values of 73.8 μM and 17.0 μM, respectively). |
|
T8491 |
Vorolanib
|
CM082,X-82 |
VEGFR
,
PDGFR
|
|
Vorolanib (X-82) is an orally active VEGFR/PDGFR dual inhibitor. |
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T2657 |
Elacridar
|
GW0918,GW120918,GF120918,GG918 |
BCRP
,
P-gp
|
|
Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor. |
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T2590 |
Vismodegib
|
Erivedge,GDC-0449,RG 3616 |
Hedgehog/Smoothened
,
ABC
,
Autophagy
|
|
Vismodegib (GDC-0449) is a hedgehog pathway inhibitor (IC50: 3 nM). It also inhibits P-gp (IC50: 3.0 μM), ABCG2 (IC50: 1.4 μM). |
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T9587 |
CCTA-1523
|
|
Others
,
ABC
|
|
CCTA-1523 is an efflux function of ABCG2 inhibitor. CCTA-1523 selectively reverses ABCG2-mediated MDR in cancer cells. |
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T2024 |
A-803467
|
A 803467,A803467 |
Sodium Channel
|
|
A-803467 is a selective NaV1.8 channel blocker. |
|
T16164 |
MY-5445
|
N-(3-chlorophenyl)-4-phenylphthalazin-1-amine |
PDE
|
|
MY-5445 (N-(3-chlorophenyl)-4-phenylphthalazin-1-amine) is a specific inhibitor of phosphodiesterase type 5 (PDE5). MY-5445 selectively inhibits cGMP PDE (Ki:1.3 μM). |
|
T5109 |
Avapritinib
|
BLU-285 |
PDGFR
,
c-Kit
|
|
Avapritinib (BLU-285) is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM). |
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T0055L |
Glafenine Hydrochloride
|
Glafenin hydrochloride |
ABC
|
|
Glafenine Hydrochloride is an anti-inflammatory agent. |
|
T16107 |
ML230
|
CID44640177,SID 88095709 |
CGRP Receptor
|
|
ML230 is a selective ATP-binding cassette (ABC) transporter ABCG2 inhibitor. It 36-fold selective for ABCG2 over ABCB1 (EC50s: 0.13 μM and 4.65 μM, respectively). |
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T33749 |
NSC107392
|
NSC 107392,NSC-107392 |
|
|
NSC107392 is a substrate of ABCG2. |
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T24552 |
NSC636795
|
NSC 636795,NSC-636795 |
|
|
NSC636795 is an ABCG2 transporter function inhibitor. |
|
T33753 |
NSC265473
|
NSC-265473,NSC-305458,NSC305458,NSC 265473,NSC 305458 |
|
|
NSC265473 is an ABCG2 substrate. |
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T25884 |
NSC103054
|
NSC-103054,NSC 103054 |
|
|
NSC103054 is an ABCG2 transporter function inhibitor. |
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T25798 |
Methyl Streptonigrin
|
NSC 45384,NSC45384,NSC-45384 |
|
|
Methyl Streptonigrin is an ABCG2 transporter function inhibitor. |
|
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 ATPas... |
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T73369 |
UR-MB108
|
|
|
|
UR-MB108 is a potent and selective inhibitor of ABCG2 (BCRP), displaying an IC50 value of 79 nM, and exhibits stability in blood plasma. |
|
T72521 |
Efflux inhibitor-1
|
|
|
|
Efflux inhibitor-1 is a pyrazolopyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC 50 s of 0.45 μM and 2.17 μM, respectively . |
|
T80245 |
LL-37(17-32)
|
|
|
|
LL-37(17-32) is a biologically active peptide fragment derived from the C-terminal domain of human cathelicidin antimicrobial peptide. This segment displays a reversal effect on ABCG2-mediated multidrug resistance in can... |
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T62432 |
KPH2f
|
|
|
|
KPH2f, a dual URAT1/GLUT9 inhibitor, demonstrates safety, oral activity, and efficacy, with inhibitory concentrations (IC50s) of 0.24 μM for URAT1 and 9.37 μM for GLUT9. It exhibits minimal effects on OAT1 and ABCG2, wit... |
|
T79711 |
Antitumor photosensitizer-4
|
|
Apoptosis
|
|
Antitumor Photosensitizer-4 (compound 10b), a conjugate of dasatinib and imatinib, serves as a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. This photosensitizer (PS) induces apoptosis and reactive oxygen speci... |
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T36485 |
Becatecarin
|
|
|
|
Becatecarin is a water-soluble, diethylaminoethyl analog of the antineoplastic antibiotic rebeccamycin. It intercalates into DNA, stabilizing the DNA-topoisomerase complex. This results in the potent catalytic inhibition... |
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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-med... |
