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Results for "

Pgp inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	P-glycoprotein (150) Akt (10) Amylases (1) Amyloid-β (1) Anaplastic lymphoma kinase (ALK) (1) Angiotensin-converting Enzyme (ACE) (1) Antibiotic (3) Apoptosis (32) Arrestin (1) Aurora Kinase (1) Autophagy (8) Bacterial (11) Bcl-2 Family (6) BCRP (17) Beta-secretase (2) Biochemical Assay Reagents (5) c-Kit (1) c-Met/HGFR (4) c-Myc (1) Calcium Channel (16) CaMK (1) Cannabinoid Receptor (1) Carbonic Anhydrase (1) Caspase (11) Cathepsin (1) CCR (1) CDK (2) CFTR (1) COX (1) Creatine Kinase (1) Cytochrome P450 (20) Deubiquitinase (1) Dopamine β-hydroxylase (2) Drug Derivative (3) Drug Isomer (1) Drug Metabolite (4) EGFR (1) Endogenous Metabolite (8) Environmental Pollutants (4) Ephrin Receptor (1) ERK (2) Ferroptosis (1) Glutathione Peroxidase (1) Glutathione S-transferase (1) Glycosidase (2) HCV Protease (1) Hedgehog (3) HIV (8) HIV Protease (9) IAP (3) iGluR (1) Isotope-Labeled Compounds (19) JNK (1) Microtubule/Tubulin (4) MMP (3) mTOR (5) NF-κB (5) NO Synthase (1) Oct3/4 (1) p38 MAPK (5) Parasite (2) PARP (4) PDGFR (1) Phosphatase (1) Phosphodiesterase (PDE) (1) PI3K (9) Potassium Channel (5) Proteasome (1) Ras (1) Reactive Oxygen Species (ROS) (6) Reference Standards (24) ROS Kinase (1) SARS-CoV (9) Serotonin Transporter (5) Somatostatin Receptor (1) STAT (3) Survivin (2) TAM Receptor (2) TNF Receptor (1) Toll-like Receptor (TLR) (4) Topoisomerase (2) Trk Receptor (4) VEGFR (3) Wee1 (2) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (150) Cardiovascular Disease (26) Infection (23) Inflammation/Immunology (16) Metabolic Disease (12) Neurological Disease (17)
Click Chemistry:	Alkynes (1)

186

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: P-glycoprotein CD44

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14275

Verapamil Maximum Cited Publications 86 Publications Verification (±)-Verapamil; CP-16533-1	Calcium Channel P-glycoprotein Cytochrome P450	Cardiovascular Disease Metabolic Disease Cancer
Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .

HY-50879

Elacridar 30+ Cited Publications GF120918; GW0918; GG918; GW120918	P-glycoprotein BCRP	Cancer
Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .

HY-10010

Ko 143 45+ Cited Publications	BCRP	Cancer
Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters .

HY-10550

Tariquidar 55+ Cited Publications XR9576	P-glycoprotein	Cancer
Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (K_d=5.1 nM) .

HY-10440

Vismodegib 50+ Cited Publications GDC-0449	Hedgehog Autophagy	Neurological Disease Inflammation/Immunology Cancer
Vismodegib (GDC-0449) is a BBB-permeable and orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits *P-gp, ABCG2* with IC₅₀ values of 3.0 μM and 1.4 μM, respectively .

HY-A0064

Verapamil hydrochloride Maximum Cited Publications 86 Publications Verification (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride	Calcium Channel P-glycoprotein Cytochrome P450	Cardiovascular Disease Cancer
Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .

HY-N6684

Deoxynivalenol 15+ Cited Publications Vomitoxin	P-glycoprotein	Metabolic Disease
Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .

HY-15255

Zosuquidar 15+ Cited Publications RS 33295-198; LY-335979	P-glycoprotein	Cancer
Zosuquidar (LY335979) is a P-glycoprotein (P-gp) inhibitor (K_i=59 nM). Zosuquidar shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research .

HY-50880

Elacridar hydrochloride 30+ Cited Publications GF120918A	P-glycoprotein BCRP	Cancer
Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer .

HY-50671

Zosuquidar trihydrochloride 15+ Cited Publications RS 33295-198 trihydrochloride; LY-335979 trihydrochloride	P-glycoprotein	Cancer
Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (K_i=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research .

HY-10550A

Tariquidar methanesulfonate, hydrate 55+ Cited Publications XR9576 methanesulfonate, hydrate	P-glycoprotein	Cancer
Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a K_d of 5.1 nM.

HY-13925

PD0166285 5+ Cited Publications	Wee1 Apoptosis	Cancer
PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC₅₀ values of 24 and 72 nM, respectively. PD0166285 exhibits an IC₅₀ of 3.433 μM for Chk1 .

HY-B1302

Quinidine hydrochloride monohydrate Maximum Cited Publications 25 Publications Verification	P-glycoprotein PARP Caspase Apoptosis Potassium Channel	Cardiovascular Disease Neurological Disease
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of *P-gp, inhibits* P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on I_K(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures .

HY-107643

Reversan CBLC4H10	P-glycoprotein	Cancer
Reversan (CBLC4H10) inhibits drug efflux mediated by P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP1), and exhibits oral activity. Reversan shows activity against glioblastoma multiforme and neuroblastoma models .

HY-17013

Dofequidar 2 Publications Verification MS-209 free base	P-glycoprotein	Cancer
Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

HY-W009141

1-Monopalmitin Glyceryl palmitate	P-glycoprotein IAP PI3K Akt Caspase Apoptosis	Cancer
1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC₅₀=50-58 μg/mL), with low toxicity to normal cells .

HY-132189

Laniquidar	P-glycoprotein	Neurological Disease
Laniquidar is a non-competitive *P-gp* inhibitor with an IC₅₀ of 0.51 μM. Laniquidar binds to the *P-gp* transporter with high affinity and exhibits low activity as a substrate. Laniquidar is applicable to epilepsy-related research .

HY-100750

Norverapamil hydrochloride 1 Publications Verification (±)-Norverapamil hydrochloride; D591 hydrochloride	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-19642A

Glesatinib hydrochloride 2 Publications Verification MGCD265 hydrochloride	TAM Receptor c-Met/HGFR	Cancer
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .

HY-D1005A25

Poloxamer 403 (P123) PEG-PPG-PEG, 5750 (Average)	Environmental Pollutants Biochemical Assay Reagents P-glycoprotein Creatine Kinase	Neurological Disease
Poloxamer 403 P123 is a block copolymer of polyoxyethylene and polyoxypropylene with an average molecular weight of 5750. Poloxamer has the ability to inhibit *P-gp. Poloxamer 403 increases creatine kinase* levels. Poloxamer 403 is myotoxic .

HY-B0501

Danofloxacin mesylate CP 76136-27	P-glycoprotein Bacterial Antibiotic	Infection
Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .

HY-17013A

Dofequidar fumarate 2 Publications Verification MS-209	P-glycoprotein	Cancer
Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .

HY-W035709

Hydrocinchonine Dihydrocinchonine	P-glycoprotein Apoptosis	Cancer
Hydrocinchonine (Dihydrocinchonine) is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of *P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic* effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp .

HY-119229

VRT-325	CFTR	Inflammation/Immunology
VRT-325 is a CFTR modulator. VRT-325 inhibits disulfide cross-linking between cysteines in transmembrane segments 6 and 7 of CFTR and *P-gp. VRT-325 promotes maturation of CFTR and P-gp* processing mutants, rescues ΔF508-CFTR folding at the endoplasmic reticulum. VRT-325 binds ΔF508-CFTR nucleotide-binding domain 1, and increases mature ΔF508-CFTR cell surface expression and chloride conductance. VRT-325 can be used for the research of cystic fibrosis ^[1] ^[3].

HY-119823

PGP-4008	P-glycoprotein	Cancer
PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin .

HY-173162

GPV0057	P-glycoprotein Potassium Channel	Cardiovascular Disease Cancer
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel K_ir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of K_ir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, K_ir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .

HY-113805

MC70	P-glycoprotein	Cancer
MC70 is a potent and non-selective P-glycoprotein (P-gp) inhibitor with an EC₅₀ of 0.69 µM. MC70 is an ABC transporters inhibitor and anticancer agent. MC70 interacts with ABCB1, ABCG2 and ABCC1 .

HY-A0064S

Verapamil-d3 hydrochloride (±)-Verapamil-d3 hydrochloride; CP-16533-1-d3 hydrochloride	Isotope-Labeled Compounds Calcium Channel P-glycoprotein Cytochrome P450	Cardiovascular Disease
Verapamil-d₃ (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .

HY-19642

Glesatinib MGCD265	TAM Receptor c-Met/HGFR	Cancer
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .

HY-10550R

Tariquidar (Standard) XR9576 (Standard)	Reference Standards P-glycoprotein	Cancer
Tariquidar (Standard) is the analytical standard of Tariquidar. This product is intended for research and analytical applications. Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM) .

HY-N4108

Hypophyllanthin	P-glycoprotein	Inflammation/Immunology Cancer
Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .

HY-132866

YS-370	P-glycoprotein	Cancer
YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .

HY-D1005A9

Poloxamer 183 (L63) PEG-PPG-PEG, 2650 (Average)	Biochemical Assay Reagents Bacterial P-glycoprotein	Infection
Poloxamer 183 L63 is a block copolymer of polyoxyethylene and polyoxypropylene with an average molecular weight of 2000. Poloxamer has the ability to inhibit *P-gp. Poloxamer 183 exhibits antimicrobial* activity and can inhibit Mycobacterium avium. Poloxamer 183 can be used as a cosmetic ingredient .

HY-101791

P-gp inhibitor 1	P-glycoprotein	Cancer
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

HY-19626

NSC23925	P-glycoprotein	Cancer
NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.

HY-175838

P-gp-IN-32	P-glycoprotein	Cancer
P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC₅₀ = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer .

HY-149277

FM04	P-glycoprotein	Cancer
FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC₅₀=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp .

HY-110377

Tariquidar dihydrochloride XR9576 dihydrochloride	P-glycoprotein	Cancer
Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (K_d=5.1 nM) .

HY-144366

P-gp inhibitor 3	P-glycoprotein	Cancer
P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel .

HY-178349

P-gp inhibitor 30	P-glycoprotein Apoptosis Autophagy	Cancer
P-gp inhibitor 30 is a potent *P-gp* inhibitor that reverses multidrug resistance in breast cancer by sensitizing resistant cells to Doxorubicin (ADM) (HY-15142). P-gp inhibitor 30 promotes apoptosis, induces autophagy, and suppresses proliferation, migration, and invasion of drug-resistant breast cancer cells when combined with ADM. P-gp inhibitor 30 inhibits breast tumor growth both in vitro and in vivo. P-gp inhibitor 30 can be used for drug-resistant breast cancer research .

HY-146391

P-gp inhibitor 4	P-glycoprotein	Cancer
P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC₅₀ of 94 nM. P-gp inhibitor 4 increases agent transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells .

HY-123384

KR30031	P-glycoprotein	Cardiovascular Disease Cancer
KR30031, a Verapamil (HY-14275) analog, is an orally active P-glycoprotein (P-gp) inhibitor. KR30031 enhances the cytotoxicity of anticancer agents by inhibiting *P-gp* with fewer cardiovascular adverse effects. KR30031 can be used to study multidrug resistance (MDR) reversal in cancer .

HY-128685

FD 12-9 Ac12Az9	P-glycoprotein BCRP	Cancer
FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of *P-gp* and BCRP, with EC₅₀s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity .

HY-107197

8-Prenylchrysin	P-glycoprotein	Cancer
8-prenylchrysin is a C8-prenylated flavonoid. 8-prenylchrysin inhibits *P-gp*. 8-prenylchrysin can be used for tumor research .

HY-135328AS

Norverapamil-d7 hydrochloride (±)-Norverapamil-d7 hydrochloride; D591-d7 hydrochloride	Isotope-Labeled Compounds Calcium Channel	Cardiovascular Disease
Norverapamil-d₇ (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-155032

P-gp inhibitor 15	P-glycoprotein	Cancer
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .

HY-W035709R

Hydrocinchonine (Standard) Dihydrocinchonine (Standard)	Reference Standards P-glycoprotein Apoptosis	Cancer
Hydrocinchonine (Dihydrocinchonine) (Standard) is the analytical standard of Hydrocinchonine (HY-W035709). This product is used for research and analytical purposes.Hydrocinchonine is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of *P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic* effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp .

HY-157483

P-gp inhibitor 18	P-glycoprotein	Cancer
P-gp inhibitor 18 (compound 6G) is a potent inhibitor of *P-gp. P-gp* inhibitor 18 inhibits rhodamine 123 efflux in the P-gp overexpressed leukemia cells, K562/Dox .

HY-161260

P-gp inhibitor 20	P-glycoprotein	Cancer
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC₅₀ value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .

HY-W854295

Phosphatidylinositol-1,2-dioctanoyl sodium PtdIns-(1,2-dioctanoyl) sodium	P-glycoprotein	Cancer
Phosphatidylinositol-1,2-dioctanoyl sodium significantly inhibits transmembrane *P-gp* transport in a reproducible, cell line-independent, and substrate-independent manner. Phosphatidylinositol-1,2-dioctanoyl sodium plays an important role in signal transduction and cell movement .

Cat. No.	Product Name

HY-L011

Membrane Transporter/Ion Channel Compound Library

2,174 compounds

Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell metabolism, ion homeostasis, signal transduction, the recognition process in the immune system, energy transduction, etc. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters. Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system, ion channels have been linked to, but not limited to, many diseases such asataxias, paralyses, epilepsies, and deafness. This indicates the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Ion channels are a major class of drug targets in drug development.

MCE designs a unique collection of 2,174 smal-molecule modulators that can be used for the research of Ion Channel and Membrane Transporter or high throughput screening (HTS) related drug discovery.

Cat. No.	Product Name	Type

HY-D1005A8

Poloxamer 181 (L61)

PEG-PPG-PEG, 2000 (Average)

Biochemical Assay Reagents

Poloxamer 181 L61 is a block polymer of polyethylene oxide and polypropylene oxide with an average molecular weight of 2000. Poloxamer has the ability to inhibit P-gp. Poloxamer 181 has antimicrobial activity and can inhibit Mycobacterium avium. Poloxamer 181 can form a thermally reversible hydrogel and is used as a food additive, and as an agent delivery carrier in cosmetics, pharmaceuticals and tissue engineering .

HY-D1005A10

Poloxamer 184 (L64)

PEG-PPG-PEG, 2900 (Average)

Biochemical Assay Reagents

Poloxamer 184 L64 is a block copolymer of polyethylene oxide and polypropylene oxide with an average molecular weight of 2900. Poloxamer has the ability to inhibit P-gp. Poloxamer 184 exhibits short-term skin toxicity, characterized by mild erythema and intradermal inflammatory reactions. Poloxamer 184 has antimicrobial activity, inhibiting 60% of Mycobacterium avium at a concentration of 1 mg/mL. Poloxamer 184 forms a thermoreversible hydrogel and is used as a food additive and as a drug delivery carrier in cosmetics and tissue engineering .

HY-D1005A25

Poloxamer 403 (P123) PEG-PPG-PEG, 5750 (Average)	Biochemical Assay Reagents
Poloxamer 403 P123 is a block copolymer of polyoxyethylene and polyoxypropylene with an average molecular weight of 5750. Poloxamer has the ability to inhibit *P-gp. Poloxamer 403 increases creatine kinase* levels. Poloxamer 403 is myotoxic .

HY-D1005A23

Poloxamer 401 (L121) PEG-PPG-PEG, 4400 (Average)	Biochemical Assay Reagents
Poloxamer 401 L121 is a block copolymer of polyethylene oxide and polypropylene oxide with an average molecular weight of 4400. Poloxamer has the ability to inhibit *P-gp. Poloxamer 401 inhibits* multiagent resistance and adjuvant activity. Poloxamer 401 can be used as a cosmetic ingredient. Poloxamer 401 can be used in nanoparticle engineering (lymphatic targeting particles) research .

HY-D1005A9

Poloxamer 183 (L63) PEG-PPG-PEG, 2650 (Average)	Biochemical Assay Reagents
Poloxamer 183 L63 is a block copolymer of polyoxyethylene and polyoxypropylene with an average molecular weight of 2000. Poloxamer has the ability to inhibit *P-gp. Poloxamer 183 exhibits antimicrobial* activity and can inhibit Mycobacterium avium. Poloxamer 183 can be used as a cosmetic ingredient .

Cat. No.	Product Name	Target	Research Area

HY-N6748

Roquefortine C 1 Publications Verification	P-glycoprotein Cytochrome P450 Bacterial c-Met/HGFR	Infection Neurological Disease Cancer
Roquefortine C is a mycotoxin that can be isolated from Penicillium species. Roquefortine C is an agonist of *P-gp* and an inhibitor of P450 3A and P450 1A. Roquefortine C can inhibit Gram-positive bacteria and also has certain neurotoxicity. Additionally, Roquefortine C can exert antitumor activity .

HY-162396

P-gp inhibitor 21	P-glycoprotein	Cancer
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6684

Deoxynivalenol 15+ Cited Publications Vomitoxin	Microorganisms Classification of Application Fields Terpenoids Sesquiterpenes Metabolic Disease Disease Research Fields Source Classification	P-glycoprotein
Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .

HY-17367

Atazanavir 10+ Cited Publications BMS-232632	Infection Structural Classification Alkaloids Classification of Application Fields Pyridine Alkaloids Endogenous metabolite Disease Research Fields Source Classification Cancer	HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Toll-like Receptor (TLR)
Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .

HY-N0217

Benzoylaconine 1 Publications Verification Benzoylaconitine; Isaconitine; Pikraconitin	Alkaloids Classification of Application Fields Other Alkaloids Ranunculaceae Other Diseases Aconitum carmichaeli Debx. Plants Disease Research Fields Source Classification	Angiotensin-converting Enzyme (ACE) Reactive Oxygen Species (ROS) Toll-like Receptor (TLR) NF-κB COX NO Synthase p38 MAPK P-glycoprotein
Benzoylaconine (Benzoylaconitine) is an orally active monoester alkaloid found in the traditional Chinese medicine Aconitum carmichaelii. Benzoylaconine is an ACE2 agonist (EC₅₀: 1.5 μM) with antihypertensive and anti-heart failure effects. Benzoylaconine inhibits TLR-induced MAPK and NF-κB pathways to exert anti-inflammatory effects. Benzoylaconine upregulates the protein levels of *P-gp, MRP2*, and has anti-tumor effects .

HY-B1302

Quinidine hydrochloride monohydrate Maximum Cited Publications 25 Publications Verification	Cardiovascular Disease Structural Classification Natural Products Classification of Application Fields Rubiaceae Cinchona calisaya Wedd. Plants Disease Research Fields Source Classification	P-glycoprotein PARP Caspase Apoptosis Potassium Channel
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of *P-gp, inhibits* P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on I_K(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures .

HY-W009141

1-Monopalmitin Glyceryl palmitate	Plants Source Classification	P-glycoprotein IAP PI3K Akt Caspase Apoptosis
1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC₅₀=50-58 μg/mL), with low toxicity to normal cells .

HY-17367A

Atazanavir sulfate 10+ Cited Publications BMS-232632 sulfate	Infection Structural Classification Alkaloids Classification of Application Fields Pyridine Alkaloids Endogenous metabolite Disease Research Fields Source Classification Cancer	HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Toll-like Receptor (TLR)
Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor with blood-brain barrier permeability. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .

HY-N0419

Quercimeritrin 2 Publications Verification Quercetin-7-O-β-D-glucopyranoside	Flavonols Structural Classification Ginkgoaceae Classification of Application Fields Metabolic Disease Plants Compositae Endogenous metabolite Ginkgo biloba Human Gut Microbiota Metabolites Flavonoids Derris scandens Disease Research Fields Source Classification	Glycosidase c-Kit MMP VEGFR Aurora Kinase
Quercimeritrin (Quercetin-7-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor (with an IC₅₀ of 79.88 μM against the Saccharomyces cerevisiae enzyme) and a *P-gp* substrate, with anti-angiogenic and antioxidant activities. Quercimeritrin does not cross the blood-brain barrier and does not inhibit cytochrome P450 enzymes. Quercimeritrin precisely binds to and inhibits the active sites of c-Kit, MMP-2, Aurora-A kinases and α-glucosidase, thereby disrupting target functions. Quercimeritrin effectively regulates postprandial blood glucose and also exhibits significant anti-angiogenic activity, which inhibits endothelial cell proliferation and microvascular growth. Quercimeritrin can be used in the research of diabetes and breast cancer .

HY-N1941

Isosinensetin	Flavonoids other families Classification of Application Fields Flavones Plants Inflammation/Immunology Disease Research Fields Source Classification	P-glycoprotein Bacterial HIV Protease Phosphatase Reactive Oxygen Species (ROS) NF-κB p38 MAPK ERK JNK Calcium Channel
Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC₅₀: 2.61 µM; K_i: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc .

HY-N1916

Coniferyl ferulate 1 Publications Verification	Classification of Application Fields Simple Phenylpropanols Phenols Polyphenols Dicerothamnus rhinocerotis Phenylpropanoids Umbelliferae Plants Disease Research Fields Source Classification Cancer	Glutathione S-transferase P-glycoprotein Apoptosis iGluR CaMK p38 MAPK Reactive Oxygen Species (ROS) Bacterial
Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC₅₀ = 0.3 μM), which downregulates *P-gp* expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus .

HY-N6748

Roquefortine C 1 Publications Verification	Infection Microorganisms Classification of Application Fields Cyclopeptides Disease Research Fields Source Classification	P-glycoprotein Cytochrome P450 Bacterial c-Met/HGFR
Roquefortine C is a mycotoxin that can be isolated from Penicillium species. Roquefortine C is an agonist of *P-gp* and an inhibitor of P450 3A and P450 1A. Roquefortine C can inhibit Gram-positive bacteria and also has certain neurotoxicity. Additionally, Roquefortine C can exert antitumor activity .

HY-N6015

Bacopasaponin C	Triterpenes Classification of Application Fields Terpenoids Scrophulariaceae Plants Disease Research Fields Bacopa monnieri (Linn.) Wettst. Source Classification Cancer	Parasite P-glycoprotein
Bacopasaponin C is an orally active natural glycoside. Bacopasaponin C can be isolated from Bacopa monniera. Bacopasaponin C inhibits Verapamil (HY-14275)-stimulated *P-gp* ATPase activity with an IC₅₀ of 57.83 μg/mL. Bacopasaponin C has antitumor activity against sarcomas. Bacopasaponin C has antiparasitic activity against Leishmania donovani .

HY-N0566

23-Hydroxybetulinic acid Anemosapogenin	Triterpenes Structural Classification other families Classification of Application Fields Terpenoids Plants Disease Research Fields Source Classification Cancer	Apoptosis Autophagy Bcl-2 Family Caspase Survivin p38 MAPK MMP
23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of *P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits* the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer .

HY-W035709

Hydrocinchonine Dihydrocinchonine	Alkaloids Other Alkaloids Rubiaceae Neolamarckia cadamba (Roxb.) Bosser Plants Source Classification	P-glycoprotein Apoptosis
Hydrocinchonine (Dihydrocinchonine) is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of *P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic* effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp .

HY-N3028

Taccalonolide B	Classification of Application Fields Schizocapsa plantaginea Hance Plants Disease Research Fields Taccaceae Steroids Cancer Source Classification	Microtubule/Tubulin
Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC₅₀ of 208 nM .

HY-N6932

Voacamine	Alkaloids other families Classification of Application Fields Metabolic Disease Plants Disease Research Fields Indole Alkaloids Source Classification	Cannabinoid Receptor P-glycoprotein PI3K Akt mTOR Apoptosis Autophagy EGFR
Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer .

HY-N4108

Hypophyllanthin	Phyllanthus urinaria Linn. Classification of Application Fields Lignans Euphorbiaceae Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields Source Classification	P-glycoprotein
Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .

HY-W035709R

Hydrocinchonine (Standard) Dihydrocinchonine (Standard)	Structural Classification Alkaloids Other Alkaloids Rubiaceae Neolamarckia cadamba (Roxb.) Bosser Plants Source Classification	Reference Standards P-glycoprotein Apoptosis
Hydrocinchonine (Dihydrocinchonine) (Standard) is the analytical standard of Hydrocinchonine (HY-W035709). This product is used for research and analytical purposes.Hydrocinchonine is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of *P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic* effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp .

HY-N144114

P-gp inhibitor 2	Classification of Application Fields Disease Research Fields Cancer	P-glycoprotein
P-gp inhibitor 2 is a potent *P-gp* inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC₅₀=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300) .

HY-N6684R

Deoxynivalenol (Standard) Vomitoxin (Standard)	Structural Classification Microorganisms Terpenoids Sesquiterpenes Source Classification	P-glycoprotein Reference Standards
Deoxynivalenol (Standard) is the analytical standard of Deoxynivalenol. This product is intended for research and analytical applications. Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .

HY-N13157

11α-O-Benzoyl-12β-O-acetyltenacigenin B	Structural Classification Marsdenia tenacissima (Roxb.) Moon Asclepiadaceae Plants Steroids Source Classification	P-glycoprotein
11α-O-Benzoyl-12β-O-acetyltenacigenin B is a P-glycoprotein (Pgp) inhibitor derived from Marsdenia tenacissima and belongs to the Tenacigenin B (HY-N1168) derivatives. 11α-O-Benzoyl-12β-O-acetyltenacigenin B can inhibit multidrug resistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of cancer .

HY-N11422R

Mycaminosyltylonolide (Standard)	Microorganisms Antibiotics Antibacterial Disease Research Source Classification	Reference Standards Antibiotic Bacterial
Deoxynivalenol (Standard) is the analytical standard of Deoxynivalenol. This product is intended for research and analytical applications. Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .

HY-W009141R

1-Monopalmitin (Standard) Glyceryl palmitate (Standard)	Plants Source Classification	Reference Standards Apoptosis P-glycoprotein PI3K IAP Caspase Akt
1-Monopalmitin (Glyceryl palmitate) (Standard) is the analytical standard of 1-Monopalmitin (HY-W009141). This product is intended for research and analytical applications. 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC₅₀=50-58 μg/mL), with low toxicity to normal cells .

HY-N4108R

Hypophyllanthin (Standard)	Phyllanthus urinaria Linn. Lignans Euphorbiaceae Phenylpropanoids Plants Source Classification	Reference Standards P-glycoprotein
Hypophyllanthin (Standard) is the analytical standard of Hypophyllanthin. This product is intended for research and analytical applications. Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .

HY-17367AR

Atazanavir sulfate (Standard) BMS-232632 sulfate (Standard)	Structural Classification Alkaloids Pyridine Alkaloids Endogenous metabolite Source Classification	Reference Standards HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite
Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM .

HY-17367R

Atazanavir (Standard) BMS-232632 (Standard)	Structural Classification Alkaloids Pyridine Alkaloids Endogenous metabolite Source Classification	Reference Standards HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite
Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .

HY-N15636

Coccinine (-)-Coccinine	Alkaloids Animals Haemanthus humilis Jacq. Other Alkaloids Plants Amaryllidaceae Source Classification	Serotonin Transporter P-glycoprotein
Coccinine ((-)-Coccinine) is a weak inhibitor of SERT (IC₅₀: 196.3 μM; K_i: 106.8 μM) and *P-gp* (IC₅₀: 0.96 mM). Coccinine exhibits significant anti-tumor activity against various cancer cell lines, such as breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Coccinine can be used in the research of tumors and neurological diseases .

HY-N6015R

Bacopasaponin C (Standard)	Triterpenes Structural Classification Terpenoids Scrophulariaceae Plants Bacopa monnieri (Linn.) Wettst. Source Classification	Reference Standards Parasite P-glycoprotein
Bacopasaponin C (Standard) is the analytical standard of Bacopasaponin C (HY-N6015). This product is intended for research and analytical applications. Bacopasaponin C is an orally active natural glycoside. Bacopasaponin C can be isolated from Bacopa monniera. Bacopasaponin C inhibits Verapamil (HY-14275)-stimulated *P-gp* ATPase activity with an IC₅₀ of 57.83 μg/mL. Bacopasaponin C has antitumor activity against sarcomas. Bacopasaponin C has antiparasitic activity against Leishmania donovani .

HY-N0566R

23-Hydroxybetulinic acid (Standard) Anemosapogenin (Standard)	Triterpenes Structural Classification other families Terpenoids Plants Source Classification	Reference Standards Apoptosis Autophagy Bcl-2 Family Caspase Survivin p38 MAPK MMP
23-Hydroxybetulinic acid (Standard) is the analytical standard of 23-Hydroxybetulinic acid (HY-N0566). This product is intended for research and analytical applications. 23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer.

HY-N16684

Clausarin	Structural Classification Rutaceae Coumarins Phenylpropanoids Plants Citrus sinensis (L.) Osbeck Source Classification	P-glycoprotein
Clausarin is a selective inhibitor of P-glycoprotein (P-gp), inhibiting P-gp-mediated drug efflux. Clausarin significantly inhibits Daunorubicin (HY-13062A) efflux in K562/R7 human leukemia cells overexpressing P-gp (with Cyclosporin A (HY-B0579) as a positive control). Clausarin can be naturally extracted from the roots of Citrus sinensis (sweet orange) and can be used in research related to overcoming multidrug resistance (MDR) in tumors .

HY-N7917

Tenacigenoside A	Apocynaceae Structural Classification Tetracyclic Triterpenoids Terpenoids Plants Source Classification	P-glycoprotein Apoptosis Bcl-2 Family
Tenacigenoside A is a multidrug resistance reversal agent and apoptosis inducer that selectively acts on P-glycoprotein and apoptosis-related proteins (BCL2, BCL-XL, BID). Tenacigenoside A exerts its key activity by regulating the expression of apoptosis-related proteins and inhibiting P-gp function, thereby inhibiting tumor cell proliferation, inducing tumor cell apoptosis, and reversing multidrug resistance in tumors. Tenacigenoside A can be used in research on malignant tumors such as lymphoma .

HY-N10342

Cajanol	Structural Classification Flavonoids Leguminosae Phenols Polyphenols Plants Isoflavones Cajanus cajan (L.) Millsp. Source Classification	Apoptosis Bcl-2 Family Caspase PARP Reactive Oxygen Species (ROS) Bacterial PI3K Akt NF-κB P-glycoprotein
Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp. . Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of *P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits* the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections .

Cat. No.	Product Name	Chemical Structure

HY-A0064S

Verapamil-d3 hydrochloride

Verapamil-d₃ (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .

HY-17367S4

Atazanavir-d6

Atazanavir-d₆ is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM .

HY-135328AS

Norverapamil-d7 hydrochloride
Norverapamil-d₇ (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-17367S2

Atazanavir-d9

Atazanavir-d₉ is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM .

HY-135328S

Norverapamil-d7
Norverapamil-d₇ is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-W699430

Norverapamil-d6 hydrochloride
Norverapamil-d₆ ((±)-Norverapamil-d₆) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-W705354

Vismodegib-d4
Vismodegib-d₄ is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits *P-gp, ABCG2* with IC₅₀ values of 3.0 μM and 1.4 μM, respectively .

HY-W716916

Vismodegib-d7
Vismodegib-d₇ is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits *P-gp, ABCG2* with IC₅₀ values of 3.0 μM and 1.4 μM, respectively .

HY-W777317

Elacridar-d4(Major)
Elacridar-d₄(Major) is the deuterium labeled Elacridar (HY-50879). Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .

HY-14275S

Verapamil-d3
Verapamil-d₃ ((±)-Verapamil-d₃) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .

HY-14275S2

Verapamil-d6
Verapamil-d₆ ((±)-Verapamil-d₆) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .

HY-14275S1

Verapamil-d7
Verapamil-d₇ is the deuterium labeled Verapamil (HY-14275). Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .

HY-17367S3

Atazanavir-d5

Atazanavir-d₅ is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM .

HY-A0064S1

Verapamil-d6 hydrochloride

Verapamil-d₆ (CP-16533-1-d₆) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .

HY-17367S5

Atazanavir-d24

Atazanavir-d₂₄ (BMS-232632-d₂₄) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .

HY-B0168BS

Levomilnacipran-d5 hydrochloride

Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .

HY-14794AS

Levomilnacipran-d10 hydrochloride

Levomilnacipran-d₁₀ ((1S,2R)-Milnacipran-d₁₀) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .

HY-W009141S

1-Monopalmitin-d31

1-Monopalmitin-d₃₁ (Glyceryl palmitate-d₃₁) is the deuterium labeled 1-Monopalmitin (HY-W009141). 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC₅₀=50-58 μg/mL), with low toxicity to normal cells .

HY-N6748S

Roquefortine C-13C22
Roquefortine C- ¹³C₂₂ is the ¹³C-labeled Roquefortine C (HY-N6748). Roquefortine C is a mycotoxin that can be isolated from Penicillium species. Roquefortine C is an agonist of P-gp and an inhibitor of P450 3A and P450 1A. Roquefortine C can inhibit Gram-positive bacteria and also has certain neurotoxicity. Additionally, Roquefortine C can exert antitumor activity .

Cat. No.	Product Name		Classification

HY-135328AS

Norverapamil-d7 hydrochloride (±)-Norverapamil-d7 hydrochloride; D591-d7 hydrochloride		Alkynes
Norverapamil-d₇ (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

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Pgp inhibitor

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