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
2775 Probucol
ABCA1 (CERP) inhibitor; also antioxidant, anti-inflammatory and hypocholesterolemic agent
4042 PSC 833
Inhibitor of P-gp-mediated MDR
6885 PU 23
Multidrug resistance protein (MRP) 4 inhibitor
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.

External sources of pharmacological information for Multidrug Transporters :

    Literature for Multidrug Transporters

    Tocris offers the following scientific literature for Multidrug Transporters to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


    Cancer

    Cancer Research Product Guide

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    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 p://> 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