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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
20 Results for "
P-glycoprotein-mediated resistance
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "P-glycoprotein-mediated resistance" in MCE Product Catalog:
3
3 Cited Publications
Synonyms: HTI-286; SPA-110
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Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis .
3
3 Cited Publications
Cat. No.: HY-15584A
CAS No.: 228266-41-9
Synonyms: HTI-286 trifluoroacetate; SPA-110 trifluoroacetate
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Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis .
3
3 Cited Publications
Cat. No.: HY-15584B
Purity: 99.34%
Synonyms: HTI-286 hydrochloride; SPA-110 hydrochloride
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Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis .
Synonyms: (1R,9R)-DX8951f
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(1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
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DpC is a selective, orally active iron chelator with anticancer activity. DpC acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer .
Synonyms: (1S,9R)-DX8951f
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Research Areas:
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia .
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
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P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
Cat. No.: HY-13776
CAS No.: 762219-35-2
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XR9051 is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR) .
Cat. No.: HY-13776A
CAS No.: 180422-22-4
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XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR) .
Cat. No.: HY-149981
CAS No.: 3041121-57-4
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P-gp inhibitor 13 is a P-gp inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia .
Cat. No.: HY-10982A
CAS No.: 150091-68-2
Synonyms: AS1413 dihydrochloride
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Amonafide dihydrochloride (AS1413 dihydrochloride) is a topoisomerase II (Topo II) inhibitor and DNA intercalator with activity in inducing apoptotic signaling. Amonafide dihydrochloride can inhibit the binding of Topo II to DNA, thereby preventing the synthesis of DNA and RNA. Amonafide dihydrochloride maintains cytotoxic activity in the presence of P-glycoprotein-mediated multidrug resistance (MDR) .
Cat. No.: HY-172771
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Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs .
Cat. No.: HY-168953
CAS No.: 3043797-88-9
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Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume .
Cat. No.: HY-171718
CAS No.: 550356-40-6
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seco-CBI-PBD dimer is a CBI-PBD heterodimer and a minor groove DNA crosslinker. seco-CBI-PBD dimer exhibits cytotoxicity against human tumor cells at sub-pM to low nM levels, shows low sensitivity to P-glycoprotein-mediated drug resistance, and can serve as an ADC payload. seco-CBI-PBD dimer can be used in studies of uterine cancer, breast cancer, non-small cell lung cancer, etc.
Cat. No.: HY-101791R
CAS No.: 2050747-49-2
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P-gp inhibitor 1 (Standard) is the analytical standard of P-gp inhibitor 1 (HY-101791). This product is intended for research and analytical applications. P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
Cat. No.: HY-117593
CAS No.: 1369591-04-7
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NSC 23925B is a P-glycoprotein (P-gp) inhibitor, as well as the most biologically active isomer of NSC23925 (HY-19626), which reverses and prevents P-glycoprotein-mediated multidrug resistance in cancer cells. NSC 23925B shows weak inhibition against most CYP450 enzymes (IC50 > 10 μM), and exhibits moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B can be used for the research of multidrug-resistant cancers .
Cat. No.: HY-183632
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QW-5-70 is a potent colchicine‑site tubulin inhibitor that blocks tubulin polymerization. QW-5-70 induces mitotic and G2/M cell cycle arrest, triggers mitochondrial apoptosis, and suppresses cancer cell colony formation and migration. QW-5-70 overcomes P‑glycoprotein‑mediated multidrug resistance and inhibits drug‑resistant tumor growth. QW-5-70 demonstrates strong in vitro and in vivo antitumor efficacy in neuroblastoma and prostate cancer models. QW-5-70 can be used for the research of high-risk neuroblastoma and castration-resistant prostate cancer .
Cat. No.: HY-114243A
CAS No.: 1382469-40-0
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Neurological Disease Inflammation/Immunology Endocrinology Cancer
DpC hydrochloride is a selective, orally active iron chelator with anticancer activity. DpC hydrochloride acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC hydrochloride induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC hydrochloride inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC hydrochloride is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer .
Cat. No.: HY-13631V
CAS No.: 2489613-15-0
Synonyms: (1R,9R)-DX-8951
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(1R,9R)-Exatecan ((1R,9R)-DX8951f) is a non-prodrug Camptothecin (HY-16560) derivative and a potent topoisomerase I (Topo I) inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan is (1S,9R)-Exatecan (HY-13631I).
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
