2. Cancer
  3. Cancer Drug Resistance

Cancer Drug Resistance

Drug resistance in chemotherapy, radiotherapy, molecular targeted therapy and immunotherapy is one of the main causes of death due to cancer. Gene mutations, non-genetic and epigenetic mechanisms to evade drug actions can promote the occurrence of drug resistance and treatment failure. Simultaneous resistance to multiple drugs with different chemical structures, different mechanisms of action and different targets is known as multidrug resistance (MDR). MDR can be related to a variety of mechanisms, including overexpression of drug efflux pumps(ABC transporter family), decreased drug uptake, mutation/loss of receptors, altered apoptotic pathway, enhanced DNA repair and drug metabolism(glutathione S-transferase, CYP450).

ABC transporters are membrane protein superfamily that can mediate MDR mechanism in many types of cancer. Some members of this superfamily includes MDR-associated protein-1(MRP1/ABCC1), breast cancer resistant proteins(ABCG2/BRCP) and P-glycoprotein(P-gp/ABCB1/MDR1). Among them, P-gp is the most extensively characterized efflux pump of MDR, and plays an important role in many cancers such as breast cancer, human lung cancer, ovarian cancer, and colorectal cancer.

The design of antitumor drugs that are able to evade or reverse MDR is rapidly evolving in the anti-cancer drug discovery field. Nanoparticle-based drug delivery platforms have been widely studied in cancer treatment, and become optimal carriers to reverse the limitations encountered in the use of traditional drug formulations, by influencing/manipulating ABC transporter-associated drug efflux mechanisms.

Cancer Drug Resistance Related Products (1940):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-133191
    Bis-propargyl-PEG2 126422-57-9
    Bis-propargyl-PEG2 is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-propargyl-PEG2 is used for the synthesis of demethylvancomycin dimers. Bis-propargyl-PEG2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Bis-propargyl-PEG2
  • HY-162633
    USP1-IN-9 2925548-22-5
    USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer.
    USP1-IN-9
  • HY-N18294
    (R,R)-Polysphorin 137196-25-9
    (R,R)-Polysphorin is a neolignan antimalarial agent that is isolated from the dried leaves and stems of Rhaphidophora decursiva. (R,R)-Polysphorin inhibits the growth of chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum clones in vitro by mediating free radical damage to key cellular components via conjugated double bonds. (R,R)-Polysphorin also exhibits cytotoxicity against human oral epidermoid carcinoma cells.
    (R,R)-Polysphorin
  • HY-181889
    KRAS G12C-IN-75
    KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRASG12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRASG12C alkylation in KRASG12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer.
    KRAS G12C-IN-75
  • HY-161521
    PLK1-IN-10 2991469-21-5
    PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death.
    PLK1-IN-10
  • HY-178466
    Tubulin polymerization/P-gp-IN-1
    Tubulin polymerization/P-gp-IN-1 is a Tubulin polymerization/P-gp dual inhibitor. Tubulin polymerization/P-gp-IN-1 inhibits tubulin polymerization and induces G2/M arrest and apoptosis. Tubulin polymerization/P-gp-IN-1 reverses MDR by inhibiting P-gp efflux function. Tubulin polymerization/P-gp-IN-1 has dual functions: direct antitumor activity and reversal of P-gp-mediated Cisplatin (HY-17394) resistance. Tubulin polymerization/P-gp-IN-1 stable binds to the tubulin CBS (ΔG = −12.4 kcal/mol) and the P-gp hydrophobic lumen (ΔG = −10.8 kcal/mol). Tubulin polymerization/P-gp-IN-1 can be used for the study of drug-resistant cervical cancer.
    Tubulin polymerization/P-gp-IN-1
  • HY-121588
    IMTPPE 851688-13-6
    IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors.
    IMTPPE
  • HY-E71367
    Bromelain (USP)
    Bromelain USP is an orally active proteolytic agent. Bromelain USP converts plasminogen to plasmin to support fibrinolysis, cleaves CD44 adhesion molecules from cell surfaces, and diminishes uPAR expression and uPA activity. Bromelain USP can inhibit the activity of a variety of fungi and bacteria. Bromelain USP can be used for the research of angina pectoris, atherosclerotic disease, fungal infections, bacterial infections, chronic inflammatory bowel disease, and cancer.
    Bromelain (USP)
  • HY-138008
    WX-132-18B 1415262-07-5
    WX-132-18B is a tubulin inhibitor with an IC50 of 0.45-0.99 nM. WX-132-18B selectively binds to the colchicine-binding site on tubulin, reduces microtubule content via depolymerization, and inhibits tubulin polymerization. WX-132-18B induces tumor cell cycle arrest, apoptosis and changes in nuclear membrane permeability, and decreases mitochondrial membrane potential. WX-132-18B exhibits antiproliferative activity against endothelial cells and human tumor cells, and inhibits the proliferation and growth of xenograft tumors in mice. WX-132-18B can be used in research related to sarcoma, non-small cell lung cancer, gastric cancer and breast cancer.
    WX-132-18B
  • HY-W230975
    (E/Z)-Piperine 7780-20-3 98.91%
    (E/Z)-Piperine ((E/Z)-Bioperine) is an alkaloid with a pungent property. (E/Z)-Piperine shows anti-inflammation, immunomodulatory and anti-cancer, antispasmodic and anti-secretory effects. (E/Z)-Piperine demonstrates significant neuroprotective effect in Alzheimer’s disease and Parkinson’s disease.
    (E/Z)-Piperine
  • HY-121247
    Bromotetrandrine 62067-29-2
    Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR). Bromotetrandrine shows significant MDR reversal activity in vitro and in vivo, which may be related to the inhibition of P-gp overexpression and the increase in intracellular accumulation of anticancer agents. Bromotetrandrine is a brominated derivative of tetrandrine, which is promising for MDR modulator for tumor assessment.
    Bromotetrandrine
  • HY-183635
    ELMO2-IN-1 1216514-48-5
    ELMO2-IN-1 is an ELMO2 inhibitor with a human target Kd of 1.0 µM. ELMO2-IN-1 binds to ELMO2, disrupting its function. ELMO2-IN-1 induces autophagy-dependent cell death. ELMO2-IN-1 can be used for the research of non-small cell lung cancer.
    ELMO2-IN-1
  • HY-16457
    Simotaxel 791635-59-1
    Simotaxel (MST 997) is an orally active derivative of the taxane class. Simotaxel binds to β-tubulin and promotes tubulin polymerization (EC₅₀ = 0.9 μM), inhibits tubulin depolymerization, and causes cell cycle arrest at the G₂-M phase. Simotaxel disrupts the formation of the mitotic spindle and triggers the caspase-dependent apoptotic pathway (apoptosis). Simotaxel has inhibitory effects on Paclitaxel (HY-B0015) sensitive cell lines and overcomes drug resistance. Simotaxel can be used to study Paclitaxel / Docetaxel (HY-B0011) resistant solid tumors.
    Simotaxel
  • HY-W740053
    Meropenem sodium 211238-34-5
    Meropenem sodium is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem sodium has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL).
    Meropenem sodium
  • HY-P11102
    Temporin-SHa 1065010-73-2
    Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.).
    Temporin-SHa
  • HY-19337S
    Ketodarolutamide-d3 2484757-41-5
    Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells. Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs. Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer.
    Ketodarolutamide-d<sub>3</sub>
  • HY-181673
    ICD inducer-2 3069681-35-9
    ICD inducer-2 is a immunogenic cell death inducer. ICD inducer-2 binds to the colchicine binding site on tubulin to inhibit tubulin polymerization. ICD inducer-2 exhibits broad-spectrum antiproliferative activity across multiple cancer cell lines. ICD inducer-2 inhibits cells migration, causes G2/M phase and induces apoptosis. ICD inducer-2 promotes infiltration of CD4+ and CD8+ T cells into the tumor microenvironment. ICD inducer-2 downregulates antiapoptotic protein Bcl-2, upregulates proapoptotic proteins Bax and Bim-1, and increases cleaved caspase 3, cleaved caspase 9, and cleaved PARP levels. ICD inducer-2 overcomes paclitaxel resistance in xenograft models and achieves tumor growth inhibition. ICD inducer-2 can be used for the research of cancer, such as lung carcinoma.
    ICD inducer-2
  • HY-161603
    EGFR/HER2-IN-14 3034701-54-4
    EGFR/HER2-IN-14 (Compd 46) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research.
    EGFR/HER2-IN-14
  • HY-E70637
    ABL1 H396P Recombinant Human Active Protein Kinase
    The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 H396P Recombinant Human Active Protein Kinase is a recombinant ABL1 H396P protein that can be used to study ABL1 H396P-related functions.
    ABL1 H396P Recombinant Human Active Protein Kinase
  • HY-151897
    HDAC-IN-49 3035173-63-5
    HDAC-IN-49 is a potent unselective HDAC (HDAC) inhibitor with IC50s of 13 nM, 14 nM, 21 nM, 1880 nM, and 10 nM for HDAC1, HDAC2, HDAC3, HDAC4, and HDAC6. HDAC-IN-49 demonstrates prominent antileukemic activity with low cytotoxic activity toward healthy cells.
    HDAC-IN-49