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ABCB1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

42

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1

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16749
    Pexidartinib
    Maximum Cited Publications
    145 Publications Verification

    PLX-3397

    		 c-Fms c-Kit Apoptosis Cancer
    Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity. Pexidartinib has limited permeability to the blood-brain barrier, primarily through ABCB1 .
    Pexidartinib
  • HY-101561
    Avapritinib
    10+ Cited Publications

    BLU-285

    		 c-Kit PDGFR Cancer
    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib
  • HY-109061
    Lazertinib
    3 Publications Verification

    YH25448; GNS-1480

    		 Apoptosis Akt TRP Channel EGFR ERK Infection Neurological Disease Metabolic Disease Cancer
    Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib
  • HY-13687
    IKK 16
    25+ Cited Publications

    		 IKK LRRK2 P-glycoprotein PKD NF-κB TNF Receptor Interleukin Related Cardiovascular Disease Inflammation/Immunology
    IKK 16 is an orally active IKK inhibitor. IKK 16 shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway .
    IKK 16
  • HY-101511
    TTT-28

    		P-glycoprotein Cancer
    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
    TTT-28
  • HY-109061B
    Lazertinib mesylate
    3 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 TRP Channel EGFR Akt ERK Apoptosis Cancer
    Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate
  • 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 .
    Dofequidar
  • HY-137433
    Befotertinib
    2 Publications Verification

    D-0316

    		 EGFR P-glycoprotein Apoptosis Cancer
    Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
    Befotertinib
  • HY-13687A
    IKK 16 hydrochloride
    25+ Cited Publications

    		 IKK LRRK2 P-glycoprotein PKD NF-κB TNF Receptor Interleukin Related Cardiovascular Disease Inflammation/Immunology
    IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway .
    IKK 16 hydrochloride
  • 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 .
    Dofequidar fumarate
  • HY-N2382
    Polyphyllin H
    1 Publications Verification

    		 Cytochrome P450 P-glycoprotein Metabolic Disease Cancer
    Polyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. Polyphyllin H potently inhibits the activities of CYP1A2 (IC50 = 6.44 μM, competitive), CYP2D6 (IC50 = 13.88 μM, competitive) and CYP3A4 (IC50 = 4.52 μM, non-competitive, time-dependent). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel .
    Polyphyllin H
  • HY-139848
    WS-898

    		P-glycoprotein Cancer
    WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).
    WS-898
  • 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 .
    MC70
  • HY-111678
    ML230

    CID44640177; SID 88095709

    		 BCRP Cancer
    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively .
    ML230
  • HY-148574
    MCT1-IN-3

    		Monocarboxylate Transporter P-glycoprotein Cancer
    MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer .
    MCT1-IN-3
  • 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 .
    YS-370
  • HY-162324
    MX106-4C

    		Survivin Cancer
    MX106-4C is a survivin inhibitor that selectively kills ABCB1-positive colorectal cancer cells. MX106-4C can exert synergistic anticancer effects with Doxorubicin or resensitize drug-resistant ABCB1 cells to Doxorubicin .
    MX106-4C
  • HY-112505
    Efflux inhibitor-1

    		BCRP Cancer
    Efflux inhibitor-1 (compound 2) is a pyrazolo[1,5-a]pyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC50s of 0.45 μM and 2.17 μM, respectively .
    Efflux inhibitor-1
  • HY-N16577
    (S)-Tenacissoside F

    		P-glycoprotein Cancer
    (S)-Tenacissoside F (Compound P20) is a polyoxypregnane compound found in Marsdenia tenacissima. (S)-Tenacissoside F can inhibit the drug efflux activity mediated by P-glycoprotein (P-gp/ABCB1) and reverse multidrug resistance. (S)-Tenacissoside F can be used for the research of cancer, such as colon cancer .
    (S)-Tenacissoside F
  • HY-174435
    ABCB1/ABCG2-IN-1

    		P-glycoprotein Cancer
    ABCB1/ABCG2-IN-1 (Compound (S,Z)-4b) is an inhibitor of ABCB1 and ABCB2 transporters. ABCB1/ABCG2-IN-1 shows moderate activity in SW620M, -V, and –Mito variants (IC50 ≈ 50 μM). ABCB1/ABCG2-IN-1 affects methotrexate resistance in vitro. ABCB1/ABCG2-IN-1 can be studied in anticancer research .
    ABCB1/ABCG2-IN-1
  • HY-137433A
    Befotertinib mesylate

    D-0316 mesylate

    		 EGFR P-glycoprotein Apoptosis Inflammation/Immunology Cancer
    Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
    Befotertinib mesylate
  • HY-168921
    ABCB1-IN-3

    		P-glycoprotein Apoptosis Cancer
    ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrug resistance (MDR) to Paclitaxel in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with Paclitaxel exhibits potent tumor suppression in vivo without generating toxicity .
    ABCB1-IN-3
  • HY-13687R
    IKK 16 (Standard)

    		IKK LRRK2 Reference Standards P-glycoprotein PKD NF-κB TNF Receptor Interleukin Related Inflammation/Immunology
    IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.
    IKK 16 (Standard)
  • HY-10320G
    Doramapimod (GMP)

    BIRB 796 (GMP)

    		 p38 MAPK Cancer
    Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity .
    Doramapimod (GMP)
  • HY-101561R
    Avapritinib (Standard)

    BLU-285 (Standard)

    		 Reference Standards c-Kit PDGFR Cancer
    Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib (Standard)
  • HY-W754911
    Avapritinib-d3

    BLU-285-d3

    		 Isotope-Labeled Compounds PDGFR c-Kit Cancer
    Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib-d3
  • HY-163981
    ABCB1-IN-2

    		P-glycoprotein Cancer
    ABCB1-IN-2 (compound 16q) is a functional inhibitor that can directly bind to the ABCB1 protein and stabilize its structure without affecting the expression and subcellular localization of ABCB1. ABCB1-IN-2 can increase the sensitivity of MCF-7/ADR cells to paclitaxel (PTX), increase the accumulation of PTX, and prevent the accumulation and excretion of luciferin Rh123 mediated by ABCB1. ABCB1-IN-2, as an ABCB1-mediated multidrug resistance (MDR) reversal agent, shows a strong ability to reverse MDR .
    ABCB1-IN-2
  • HY-149366
    ABCB1-IN-1

    		P-glycoprotein Cancer
    ABCB1-IN-1 (compound 3) is a potent ABCB1 inhibitor. ABCB1-IN-1 induces cell apoptosis. ABCB1-IN-1 bearing 1-benzylimidazole has IC50 values of 1.26 μM and 2.21 μM for Colo205 and Colo320 cells, respectively .
    ABCB1-IN-1
  • HY-17648
    MBL-II-141

    		BCRP Cancer
    MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers .
    MBL-II-141
  • HY-168944
    ABCB1-IN-4

    		Amylases Glycosidase Metabolic Disease
    ABCB1-IN-4 (Compound C6z) is an orally active and potent dual α-amylase and α-glucosidase inhibitor with IC50 values of 1.63 μM and 0.14 μM, respectively. ABCB1-IN-4 is promising for research of diabetes .
    ABCB1-IN-4
  • HY-162714
    C3N-Dbn-Trp2

    		P-glycoprotein Cancer
    C3N-Dbn-Trp2 is an inhibitor for ATP-binding cassette transporter ABCB1. C3N-Dbn-Trp2 inhibits the ABCB1-mediated Rhodamine 123 (HY-D0816) efflux in cells HEK293T and HCT-15 with IC50 of 5.9 µM and 2.2 µM. C3N-Dbn-Trp2 inhibits the Doxorubicin (HY-15142A) efflux, enhances the cytotoxicity of Doxorubicin in ABCB1-expressing cells .
    C3N-Dbn-Trp2
  • HY-136934
    Reversin 205

    [Boc-Glu(Obzl)]2-Lys-Ome

    		 P-glycoprotein Cancer
    Reversin 205 ([Boc-Glu(Obzl)]2-Lys-Ome) is a P-glycoprotein (ABCB1) inhibitor. Reversin 205 is a peptide chemosensitizer .
    Reversin 205
  • HY-10550B
    Tariquidar dimesylate

    XR9576 dimesylate

    		 P-glycoprotein Cardiovascular Disease Others
    Tariquidar dimesylate (XR9576 dimesylate) is a P-glycoprotein (P-gp) inhibitor. Tariquidar dimesylate increases the concentration of the drug in the brain by binding to P-glycoprotein, preventing it from transporting the drug from inside to outside the brain. Tariquidar dimesylate can be used in the study of blood-brain barrier penetration and multidrug resistance .
    Tariquidar dimesylate
  • HY-150565
    P-gp inhibitor 5

    		P-glycoprotein Cancer
    P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015) .
    P-gp inhibitor 5
  • HY-17013D
    Dofequidar sesquifumarate

    MS-209 sesquifumarate

    		 P-glycoprotein Cancer
    Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate 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 .
    Dofequidar sesquifumarate
  • HY-182253
    WS-691

    		P-glycoprotein Cancer
    WS-691 is an orally active, selective ABCB1 modulator. WS-691 selectively stabilizes ABCB1 via direct binding to ABCB1. WS-691 inhibits the efflux function of ABCB1 and activates ABCB1 ATPase activity. WS-691 elevates intracellular Paclitaxel (HY-B0015) levels and reduces the required dose of Paclitaxel in cancer cells overexpressing ABCB1. WS-691 increases the sensitivity of colon cancer cells to Paclitaxel .
    WS-691
  • HY-101511R
    TTT-28 (Standard)

    		P-glycoprotein Reference Standards Cancer
    TTT-28 (Standard) is the analytical standard of TTT-28 (HY-101511). This product is intended for research and analytical applications. TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
    TTT-28 (Standard)
  • HY-109061A
    Lazertinib mesylate hydrate

    YH25448 mesylate hydrate; GNS-1480 mesylate hydrate

    		 Apoptosis Akt TRP Channel EGFR ERK Cancer
    Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate hydrate
  • HY-180357
    Graviquinone

    		Checkpoint Kinase (Chk) Reactive Oxygen Species (ROS) DNA/RNA Synthesis Cancer
    Graviquinone is a Chk1 inhibitor. Graviquinone exhibits potent cytotoxicity against various cancer cell lines. Graviquinone possesses the characteristics of bypassing ABCB1-mediated multidrug resistance, selectively damaging cancer cell DNA, and regulating the DNA damage response. Graviquinone can also enhance cytotoxicity by increasing ROS levels in cancer cells. Graviquinone can be used for cancer research .
    Graviquinone
  • HY-17013AR
    Dofequidar fumarate (Standard)

    MS-209 (Standard)

    		 P-glycoprotein Reference Standards Cancer
    Dofequidar (fumarate) (Standard) is the analytical standard of Dofequidar (fumarate). This product is intended for research and analytical applications. 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 .
    Dofequidar fumarate (Standard)
  • HY-13774
    WK-X-34

    		P-glycoprotein BCRP Cancer
    WK-X-34 is a low-toxicity, highly effective multidrug resistance reversal agent. By potently inhibiting the transport functions of P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP), WK-X-34 significantly increases the intracellular accumulation of anticancer drugs and radiotracers in drug-resistant cells. WK-X-34 exerts no significant effect on MRP transporters. WK-X-34 not only restores the chemosensitivity of multidrug-resistant ovarian cancer cells, but also significantly enhances the uptake of 99mTc-Sestamibi in P-gp-positive xenograft tumors, brain and intestinal tissues. WK-X-34 exhibits extremely low toxicity and favorable safety profiles both in vitro and in mice (at doses up to 50 mg/kg), and can be used for research on overcoming multidrug resistance in ovarian cancer .
    WK-X-34
  • HY-181629A
    ZSTK3744 hydrochloride

    		Aryl Hydrocarbon Receptor Apoptosis Caspase Cytochrome P450 Cancer
    ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer .
    ZSTK3744 hydrochloride

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