Multidrug Transporters

ATP-binding cassette (ABC) transporters form one of the largest groups of paralogous protein families that have a wide diversity of functions and substrates. Specificity has been shown for small and large molecules, highly charged molecules and highly hydrophobic systems.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
5867 Ceefourin 1
Selective MRP4 inhibitor
4193 CP 100356 hydrochloride
P-gp inhibitor
4646 Elacridar hydrochloride
P-gp inhibitor
3588 Estropipate
Estrogen receptor agonist and OATP1B1 inhibitor
2876 Fumitremorgin C
Inhibitor of BCRP-mediated multidrug resistance
3241 Ko 143
Potent and selective BCRP inhibitor
4169 KS 176
Selective BCRP inhibitor
2338 MK 571
MRP1 inhibitor; also CysLT1 (LTD4) inverse agonist
4107 Probenecid
MRP inhibitor
4042 PSC 833
Inhibitor of P-gp-mediated MDR
3918 Pyrimethamine
Potent inhibitor of multidrug and toxin extrusion (MATE) transporters; also DHFR and STAT3 inhibitor
3722 Reversan
Selective MRP1 and P-gp inhibitor
5757 Tariquidar dihydrochloride
Potent P-glycoprotein (P-gp) inhibitor
5456 Zosuquidar trihydrochloride
High affinity P-gp inhibitor

Substrates

Cat No Product Name / Activity
4936 Clozapine N-oxide
Metabolite of clozapine (Cat. No. 0444); shown to be a P-gp efflux pump substrate
6329 Clozapine N-oxide dihydrochloride
Water soluble salt of Clozapine N-oxide (Cat. No. 4936); shown to be a P-gp efflux pump substrate

Other

Cat No Product Name / Activity
5119 Calcein AM
Substrate for MDR
4054 PEP 005
Substrate for MDR; also protein kinase C activator

ATP-binding cassette (ABC) transporters form one of the largest groups of paralogous protein families that have a wide diversity of functions and substrates. Specificity has been shown for small and large molecules, highly charged molecules and highly hydrophobic molecule systems such as that for polysaccharides. Multidrug transporters (MDRs) are a specific type of ABC transporter and are commonly overexpressed in cancer cells.

P-glycoprotein (P-gp, ABCB1, MDR1) is a well-characterized human ABC transporter that was the first ABC transporter implicated in multidrug resistance. Normal physiological expression of P-glycoprotein has been found to prevent uptake of some lipophilic drugs into the brain and other key organs. P-glycoprotein is frequently overexpressed in cancer cells resulting in drugs being pumped out of the cells faster than they can enter. This causes a lower concentration of the drug in the cell and reduces the effectiveness of the drugs in killing cancer cells. Due to the role of P-gp in extruding xenobiotics from a broad range of cells, this transporter also confers the multidrug resistance phenotype in many different cell types.

Members of the multidrug resistance protein (MRP) family and P-gp also help maintain the integrity of the blood-brain-barrier, often preventing the entry of drugs or removing them from the CNS. This can pose a problem in therapies for CNS disorders, particularly the treatment of brain tumors.

Drugs that are affected by classical multidrug resistance include the vinca alkaloids (vinblastine and vincristine), the anthracyclines (doxorubicin and daunorubicin), the RNA transcription inhibitor actinomycin D and the microtubule-stabilizing drug taxol.

Literature for Multidrug Transporters

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Programmed Cell Death

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Multidrug Transporter Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
ABCA1 Human ABCA1 NM_005502 Q9UN09
Mouse Abca1 NM_013454 P41233
Rat Abca1 NM_178095 Q80ZB2
ABCA2 Human ABCA2 NM_001606 Q9BZC7
Mouse Abca2 NM_007379 P41234
Rat Abca2 NM_024396 Q9ESR9
ABCA3 Human ABCA3 NM_001089 Q99758
Mouse Abca3 NM_013855 Q8R420
Rat Abca3 XM_220219 Q5M866
ABCA4 Human ABCA4 NM_000350 P78363
Mouse Abca4 NM_007378 O35600
Rat Abca4 NM_001107721 XP_241525
ABCA5 Human ABCA5 NM_172232 Q8WWZ7
Mouse Abca5 NM_147219 Q8K448
Rat Abca5 NM_173307 Q8CF82
ABCA6 Human ABCA6 NM_080284 Q8N139
Mouse Abca6 NM_147218 Q8K441
Rat Abca6 XM_001081607 XP_001081607
ABCA7 Human ABCA7 NM_019112 Q8IZY2
Mouse Abca7 NM_013850 Q91V24
Rat Abca7 NM_207598 Q7TNJ2
ABCA8 Human ABCA8 NM_007168 O94911
Mouse Abca8b NM_013851 Q8K440
Rat Abca8 XM_221074 XP_221074
ABCA9 Human ABCA9 NM_172386 Q8IUA7
Mouse Abca9 NM_147220 Q8K449
Rat Abca9 XM_221101 XP_221101
ABCA10 Human ABC10 NM_080282 Q8WWZ4
ABCA12 Human ABCA12 NM_173076 Q86UK0
Mouse Abca12 BC158053 B2RY11
Rat Abca12 XM_237242 XP_237242
ABCA13 Human ABCA13 NM_152701 Q86UQ4
Mouse Abca13 NM_178259 Q5SSE9
Rat Abc13 NM_001106020 XP_223625
ABCB1 (P-gp, MDR1) Human ABCB1 NM_000927 P08183
Mouse Abcb1a NM_011076 P21447
Rat Abcb1 NM_133401 Q9JK64
ABCB4 Human ABCB4 NM_000443 P21439
Mouse Abcb4 NM_008830 P21440
Rat Abcb4 NM_012690 Q64714
ABCB5 Human ABCB5 NM_178559 Q2M3G0
Mouse Abcb5 NM_029961 NP_084237
Rat Abcb5 XM_234725 XP_234725
ABCB6 Human ABCB6 NM_005689 Q9NP58
Mouse Abcb6 NM_023732 Q9DC29
Rat Abcb6 NM_080582 O70595
ABCB7 Human ABCB7 NM_004299 O75027
Mouse Abcb7 NM_009592 Q61102
Rat Abcb7 NM_212518 Q704E8
ABCB8 Human ABCB8 NM_007188 Q9NUT2
Mouse Abcb8 NM_029020 Q9CXJ4
Rat Abcb8 NM_001007796 Q5RKI8
ABCB9 Human ABCB9 NM_203444 Q9NP78
Mouse Abcb9 NM_019875 Q9JJ59
Rat Abcb9 NM_022238 Q764Q6
ABCB10 Human ABCB10 NM_012089 Q9NRK6
Mouse Abcb10 NM_019552 Q9JI39
Rat Abcb10 NM_001012166 Q5FVL8
ABCB11 Human ABCB11 NM_003742 O95342
Mouse Abcb11 NM_021022 Q9QY30
Rat Abcb11 NM_031760 O70127
ABCC1 (MRP1) Human ABCC1 NM_019862 P33527
Mouse Abcc1 NM_008576 O35379
Rat Abcc1 NM_022281 Q8CG09
ABCC2 (MRP2) Human ABCC2 NM_000392 Q92887
Mouse Abcc2 NM_013806 Q8VI47
Rat Abcc2 NM_012833 Q63120
ABCC3 (MRP3) Human ABCC3 NM_020038 O15438
Mouse Abcc3 NM_029600 B2RX12
Rat Abcc3 NM_080581 O88563
ABCC4 (MRP4) Human ABCC4 NM_005845 O15439
Mouse Abcc4 NM_001033336 NP_001028508
Rat Abcc4 NM_133411 Q59DL1
ABCC5 (MRP5) Human ABCC5 NM_005688 O15440
Mouse Abcc5 NM_013790 Q9R1X5
Rat Abcc5 NM_053924 Q9QYM0
ABCC6 (MRP6) Human ABCC6 NM_001079528 O95255
Mouse Abcc6 NM_018795 Q9R1S7
Rat Abcc6 NM_031013 O88269
CFTR Human CFTR NM_000492 P13569
Mouse Cftr NM_021050 P26361
Rat Cftr NM_031506 P97522
ABCC8 (MRP8) Human ABCC8 NM_000352 Q09428
Mouse Abcc8 NM_011510 NP_035640
Rat Abcc8 NM_013039 Q09429
ABCC9 Human ABCC9 NM_005691 O60706
Mouse Abcc9 NM_021041 P70170
Rat Abcc9 NM_013040 Q9QWX3
ABCC10 Human ABCC10 NM_033450 Q5T3U5
Mouse Abcc10 NM_145140 Q8R4P9
Rat Abcc10 NM_001108201 XP_236930
ABCC11 Human ABCC11 NM_032583 Q96J66
ABCC12 Human ABCC12 NM_033226 Q96J65
Mouse Abcc12 NM_172912 Q80WJ6
Rat Abcc12 NM_199377 Q6Y306
ABCC13 Human ABCC13 NR_003088 Q9NSE7
ABCD1 Human ABCD1 NM_000033 P33897
Mouse Abcd1 NM_007435 P48410
Rat Abcd1 NM_001108821 XP_343841
ABCD2 Human ABCD2 NM_005164 Q9UBJ2
Mouse Abcd2 NM_011994 Q61285
Rat Abcd2 NM_033352 Q9QY44
ABCD3 Human ABCD3 NM_002858 P28288
Mouse Abcd3 NM_008991 P55096
Rat Abcd3 NM_012804 P16970
ABCD4 Human ABCD4 NM_005050 O14678
Mouse Abcd4 NM_008992 O89016
Rat Abcd4 NM_001013100 Q5FWT4
ABCE1 Human ABCE1 NM_002940 P61221
Mouse Abce1 NM_015751 P61222
Rat Abce1 NM_001108446 XP_341670
ABCF1 Human ABCF1 NM_001025091 Q8NE71
Mouse Abcf1 NM_013854 Q6P542
Rat Abcf1 NM_001109883 Q6MG08
ABCF2 Human ABCF2 NM_007189 Q9UG63
Mouse Abcf2 NM_013853 Q99LE6
Rat Abcf2 NM_001109666 XP_231307
ABCF3 Human ABCF3 NM_018358 Q9NUQ8
Mouse Abcf3 NM_013852 Q8K268
Rat Abcf3 NM_001011896 Q66H39
ABCG1 Human ABCG1 NM_207174 Q9BXL1
Mouse Abcg1 NM_009593 Q64343
Rat Abcg1 NM_053502 Q9EPG9
ABCG2 (BCRP) Human ABCG2 NM_004827 Q8IX16
Mouse Abcg2 NM_011920 Q7TMS5
Rat Abcg2 NM_181381 Q80W57
ABCG3 Mouse Abcg3 NM_030239 Q99P81
Rat Abcg3 NM_001128311 XP_573551
ABCG4 Human ABCG4 NM_022169 Q9H172
Mouse Abcg4 NM_138955 NP_620405
Rat Abcg4 NM_001106816 XP_236186
ABCG5 Human ABCG5 NM_022436 Q9H222
Mouse Abcg5 NM_031884 Q99PE8
Rat Abcg5 NM_053754 Q923R8
ABCG8 Human ABCG8 NM_022437 Q9H221
Mouse Abcg8 NM_026180 Q9DBM0
Rat Abcg8 NM_130414 P58428
SLC47A1 Human SLC47A1 NM_018242 Q96FL8
Mouse Slc47a1 NM_026183 Q8K0H1
SLC47A2 Human SLC47A2 NM_152908 AB250364