ATP-binding cassette (ABC) transporters

ATP-binding cassette transporters

ATP-binding cassette (ABC) transporters are a large group of membrane proteins, comprising 49 transporters that are further subdivided into seven subfamilies, ABC A to G, based on sequence similarities, that have two nucleotide-binding domains (NBDs) and two transmembrane binding domains (TMDs). ATP-binding cassette (ABC) transporters couple transport of a substrate against a chemical gradient and energized directly by the hydrolysis of ATP. ATP-binding cassette transporters transport a wide variety of substrates, including inorganic and organic small molecules like metal ions, sugars, amino acids, nucleotides, and vitamins, as well as larger organic compounds such as peptides, proteins, oligonucleotides, cellular metabolites, and drugs. ATP-binding cassette (ABC) transporters are involved in many important physiological processes like nutrient uptake, cellular detoxification, lipid homeostasis, signal transduction, viral defense, and antigen presentation. ATP-binding cassette (ABC) transporters play an important role in a number of diseases, including Stargardt disease, Alzheimer's disease, immune deficiency, and cystic fibrosis^[1]^[2].

References:

[1]. Locher KP. Review. Structure and mechanism of ATP-binding cassette transporters. Philos Trans R Soc Lond B Biol Sci. 2009 Jan 27;364(1514):239-45. [Content Brief]

[2]. Sodani K, et al. Multidrug resistance associated proteins in multidrug resistance. Chin J Cancer. 2012 Feb;31(2):58-72. [Content Brief]

ATP-binding cassette (ABC) transporters Related Products (19):

By Effects:	Inhibitors (3) Substrate (1) Activators (5) Modulators (3) Inducers (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-W585842

Estradiol 3-glucuronide		98.00%
Estradiol 3-glucuronide is an estrogen metabolite, which is a glucuronide conjugate formed from Estradiol (HY-B0141) via catalysis by uridine diphosphate glucuronosyltransferases in tissues such as the liver. Estradiol 3-glucuronide is a potent substrate of Mrp2, with an S₅₀ value of 55.7 μM. Estradiol 3-glucuronide achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP.

HY-W010649

Isoxazole	Inhibitor	99.98%
Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor.

HY-183033

ABC transporter modulator-2	Activator
ABC transporter modulator-2 (Compound I-200) is a ABC transporter expression modulator. ABC transporter modulator-2 upregulates the expression of wild-type ABCC6 with an EC₅₀ of <1 μM. ABC transporter modulator-2 upregulates the expression of wild-type ABCB4 with an EC₅₀ of <1 μM. ABC transporter modulator-2 upregulates the expression of wild-type ABCD2 with an EC₅₀ of <1 μM. ABC transporter modulator-2 upregulates the expression of the ABCA4^P1380L mutant with an EC₅₀ of <1 μM. ABC transporter modulator-2 can be used in the research of diseases associated with ABC transporter dysfunction.

HY-183032

ABC transporter modulator-1	Activator
ABC transporter modulator-1 (Compound I-5) is an ABC transporter expression enhancer. ABCC6 modulator-1 upregulates the expression of wild-type ABCC6, wild-type ABCB4, and ABCA4^P1380L mutant, with an EC₅₀ of <1 μM for all.

HY-183034

ABC transporter modulator-3	Activator
ABCC6 modulator-3 (Compound I-71) is a ABCC6 activator with an EC₅₀ < 1 μM. ABCC6 modulator-3 upregulates the expression of wild-type ABCC6. ABCC6 modulator-3 is used in research on diseases associated with ABC transporter dysfunction.

HY-W674245

10-Hydroxyhexadecanoic acid		98.91%
10-Hydroxyhexadecanoic acid is a hydroxy fatty acid found in Camembert cheese. 10-Hydroxyhexadecanoic acid can promote cholesterol efflux from ABCA1 and ABCG1, preventing the accumulation of excess cholesterol in cells. 10-Hydroxyhexadecanoic acid can be used in anti-atherosclerosis research.

HY-173230

ABCA1 inducer 2	Inducer	98.22%
ABCA1 inducer 2 is a non-lipotropic ABCA1 inducer. ABCA1 inducer 2 upregulates the expression of ABCA1 by targeting the LXR pathway. ABCA1 inducer 2 can reduce ox-LDL-induced lipid accumulation and thus inhibit foam cell formation. ABCA1 inducer 2 has anti-atherosclerotic potential.

HY-137307

Cholest-5-ene-3ß,22(S)-diol	Inducer	98.69%
Cholest-5-ene-3ß,22(S)-diol ((22S)-Hydroxycholesterol) is an orally active oxysterol with no significant cytotoxic, oxidative, or inflammatory effects on human prokaryotic leukemia cells. Cholest-5-ene-3ß,22(S)-diol inhibits weight gain and increased serum triacylglycerol (TAG) levels in rat models.

HY-N7755

Estradiol 3-glucuronide sodium	Substrate	98%
Estradiol 3-glucuronide sodium is an estrogen metabolite, which is a glucuronide conjugate formed by the catalysis of uridine diphosphate glucuronosyltransferase in tissues such as the liver from Estradiol (HY-B0141). Estradiol 3-glucuronide sodium is a potent substrate of Mrp2, with an S₅₀ of 55.7 μM. Estradiol 3-glucuronide sodium achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP.

HY-W010649R

Isoxazole (Standard)	Inhibitor
Amfenac (Sodium Hydrate) (Standard) is the analytical standard of Amfenac (Sodium Hydrate). This product is intended for research and analytical applications. Amfenac Sodium Hydrate is a COX-2 inhibitor.

HY-P990325

Anti-ABCB5 Antibody
Anti-ABCB5 Antibody is a CHO-expressed human antibody that targets ABCB5. The Anti-ABCB5 Antibody has a huIgG2 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-ABCB5 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

HY-120432

CaMdr1p-IN-1	Inhibitor
CaMdr1p-IN-1 (Compound A) is an inhibitor for the major facilitator superfamily transporter CaMdr1p. CaMdr1p-IN-1 exhibits chemosensitizing efficacy. CaMdr1p-IN-1 synergizes with Fluconazole (HY-B0101), that inhibits CaMdr1p overexpressing Candida albicans with MIC of 10 μM.

HY-183035

ABC transporter modulator-4	Modulator
ABC transporter modulator-4 (I-677-Isomer 1 (S configuration)) is a ABC transporter expression modulator. ABC transporter modulator-4 is used in studies of ABC transporter dysfunction.

HY-186045

SKLB06489	Activator
SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC₅₀ values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC).

HY-115780

E17110
E17110 is a liver X receptor β (LXRβ) agonist with an EC₅₀ of 0.72 μM. E17110 can increase the expression of ATP-binding cassette transporter A1 (ABCA1) and G1 (ABCG1) in RAW264.7 macrophages. E17110 also reduce cellular lipid accumulation and promoted cholesterol efflux. E17110 can be used for the research of cardiovascular disease, such as atherosclerosis.

HY-183036

ABC transporter modulator-5	Modulator
ABC transporter modulator-5 (I-677-Isomer 2 (R configuration)) is a ABC modulator. ABC transporter modulator-5 is used in studies of ABC dysfunction.

HY-181509

TNF-α/IL-1β/IL-6-IN-1	Modulator
TNF-α/IL-1β/IL-6-IN-1 is an anti-inflammatory agent. TNF-α/IL-1β/IL-6-IN-1 exerts anti-inflammatory effects by downregulating the expression of pro-inflammatory cytokines such as TNF-α, IL-1β and IL-6, and inhibiting the production of ROS. TNF-α/IL-1β/IL-6-IN-1 upregulates ABCG1 to promote cholesterol efflux. TNF-α/IL-1β/IL-6-IN-1 can be used in the research of inflammatory and lipid metabolic diseases such as atherosclerosis.

HY-117555

4010B-30	Activator
4010B-30 is a upregulator of apolipoprotein A-I (ApoA-I). 4010B-30 regulates ApoA-I gene expression through activation of PPARγ. 4010B-30 promotes cholesterol efflux and ABCA1 expression. 4010B-30 protects against atherosclerotic lesion development in ApoE^-/- mice.

HY-181520

ABCA1 inducer 3	Inducer
ABCA1 inducer 3 (Compound 85) is an orally active ABCA1 inducer and lipid-modulating agent. ABCA1 inducer 3 increases ABCA1 expression. ABCA1 inducer 3 upregulates hepatic Abcg5 and Abcg8 mRNA expression. ABCA1 inducer 3 promotes cholesterol efflux. ABCA1 inducer 3 improves hyperlipidemia.

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