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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[1] .
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 [1] .
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 [1] .
Vincristine (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) is a microtubule inhibitor that disrupts microtubule polymerization by binding to β-tubulin (with a Ki of 85 nM in bovine), arrests the cell cycle and induces apoptosis. Vincristine inhibits cell replication, tumor blood flow and the proliferation of various cancer cells, while triggering effects such as oxidative stress, inflammation, calcium overload, epithelial-mesenchymal transition and peripheral neuropathic pain. Vincristine upregulates the expression of various transporters and nuclear receptors, and enriches gastric cancer stem-like cells. Vincristine is used in research related to various tumors including acute lymphoblastic leukemia, lymphoma, melanoma, gastric cancer, solid tumors and sarcomas [1] .
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 [1] .
N-Desethyl Sunitinib (SU-12662) is a metabolite of Sunitinib (HY-10255A). N-Desethyl Sunitinib serves as a good transport substrate for human ABCB1, ABCG2 and murine ABCG2 [1] .
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[1].
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 [1] .
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 [1] .
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 [1] .
24-Epicastasterone (24-epi-Castasterone) is a bioactive brassinosteroid and a ligand of ABCB1 and ABCB19 in Arabidopsis thaliana. 24-Epicastasterone stimulates the ATPase activity of ABCB19 and the ATP hydrolysis activity of ABCB1, which drive the efflux of substances from plant cells. 24-Epicastasterone increases the activities of catalase and guaiacol peroxidase in the roots of wheat seedlings. 24-Epicastasterone alleviates heat-induced lipid peroxidation through a ROS-dependent mechanism and enhances the heat tolerance of common wheat seedlings[1].
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 [1] .
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 [1] .
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 [1] .
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).
Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin [1].
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[1] .
WS-917 is a potent and orally active ABCB1 modulator. WS-917 enhances ABCB1 ATPase activity. WS-917 significantly enhances the antitumor effect of paclitaxel combined with anti-PD-1 antibody. WS-917 promotes CD8 + T-cell activation [1].
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 [1].
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 [1].
UR-MB108 is a selective ABCG2 inhibitor with an IC50 value of 79 nM. UR-MB108 acts as a potent inhibitor of ABCG2 transport and ATPase activity. UR-MB108 can be used in cancer-related research [1].
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 [1].
ABCB1 Human Pre-designed siRNA Set A contains three designed siRNAs for ABCB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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 [1].
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 [1].
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 [1].
(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 [1].
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 [1].
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 [1].
BODIPY FL Verapamil hydrochloride is a fluorescent dye, it can be used as a molecular probe to label tissues and cells. BODIPY FL Verapamil hydrochloride is a substrate for both ABCB1 and ABCC1[1] .
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 [1].
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 [1] .
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 [1].
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.
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 [1].
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 [1] .
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 [1] .
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 [1] .
N,N-Dimethyl-idarubicin, an Idarubicin (HY-17381) derivative, is a potent histone evictor which does not induce DNA double-strand breaks. N,N-Dimethyl-idarubicin, an anthracycline, is an effective cytotoxic agent for ABCB1-overexpressing, Doxorubicin-resistant cells [1].
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 [1].
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-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015) [1].
Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma [1].
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 [1].
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 [1] .
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 [1] .
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[1].
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 [1] .
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 [1].
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 [1] .
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 [1].
ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 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 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer [1].
Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer [1] .
DB-310 is a selective immunoproteasome LMP2 inhibitor with an IC50 value of 80.62 nM. DB-310 inhibits the production of IL-1α in microglia. DB-310 improves cognitive function in the Tg2576 transgenic mouse model of Alzheimer's disease. DB-310 can be used for research related to Alzheimer's disease [1].
ProAlk01 is a protein alkylating agent that serves as a toxin payload for ADCs. ProAlk01 localizes to the cytoplasm and exerts cytotoxic effects mainly by alkylating cytoplasmic proteins rather than binding to DNA. ProAlk01 induces cell cycle arrest, apoptosis, and immunogenic cell death. ProAlk01 can be used in the research of solid tumors [1].
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 [1].
BODIPY FL Verapamil hydrochloride is a fluorescent dye, it can be used as a molecular probe to label tissues and cells. BODIPY FL Verapamil hydrochloride is a substrate for both ABCB1 and ABCC1[1] .
Vincristine (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) is a microtubule inhibitor that disrupts microtubule polymerization by binding to β-tubulin (with a Ki of 85 nM in bovine), arrests the cell cycle and induces apoptosis. Vincristine inhibits cell replication, tumor blood flow and the proliferation of various cancer cells, while triggering effects such as oxidative stress, inflammation, calcium overload, epithelial-mesenchymal transition and peripheral neuropathic pain. Vincristine upregulates the expression of various transporters and nuclear receptors, and enriches gastric cancer stem-like cells. Vincristine is used in research related to various tumors including acute lymphoblastic leukemia, lymphoma, melanoma, gastric cancer, solid tumors and sarcomas [1] .
24-Epicastasterone (24-epi-Castasterone) is a bioactive brassinosteroid and a ligand of ABCB1 and ABCB19 in Arabidopsis thaliana. 24-Epicastasterone stimulates the ATPase activity of ABCB19 and the ATP hydrolysis activity of ABCB1, which drive the efflux of substances from plant cells. 24-Epicastasterone increases the activities of catalase and guaiacol peroxidase in the roots of wheat seedlings. 24-Epicastasterone alleviates heat-induced lipid peroxidation through a ROS-dependent mechanism and enhances the heat tolerance of common wheat seedlings[1].
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 [1] .
Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin [1].
(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 [1].
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 [1] .
ABC20; ABCB1; ATP binding cassette, sub family B(MDR/TAP), member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; PGY1.
IHC-P, IF-Tissue, IHC-F, WB
Human, Mouse, Rat
P Glycoprotein Antibody (YA6354) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to P Glycoprotein.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
IHC-P, WB, ICC/IF, ELISA
Human, Mouse
P Glycoprotein Antibody (YA5626) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to P Glycoprotein.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
IHC-P, ELISA
Human, Mouse
P Glycoprotein Antibody (YA5747) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to P Glycoprotein.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
WB, IHC-P, ICC/IF, IP, ELISA
Human
P Glycoprotein Antibody (YA6028) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to P Glycoprotein.
ABCB1 Human Pre-designed siRNA Set A contains three designed siRNAs for ABCB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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