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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
1307 Results for "
moPrPC mutants
" in MedChemExpress (MCE) Product Catalog:
Products (1307)
1307 Results for "moPrPC mutants" in MCE Product Catalog:
Cat. No.: HY-175870A
CAS No.: 3024878-21-2
(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRAS G12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer .
Cat. No.: HY-179433
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PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
Cat. No.: HY-184408
CAS No.: 3033990-94-9
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AAP-SO2 is a Bactericide and Mycobacterium tuberculosis RNA polymerase (Mtb RNAP) inhibitor, with an IC50 of 0.025 μM against Mtb RNAP. AAP-SO2 allosterically slows the nucleotide addition rate during transcriptional elongation and enhances transcription termination efficiency. AAP-SO2 exhibits increased activity against β S450L-type Mtb, possesses activity against non-replicating Mtb, and shows whole-cell activity against Mtb and related mycobacterial species. AAP-SO2 reduces the overall emergence rate of Rifampicin (HY-B0272) tolerance in Mtb, alters the mutation spectrum, and decreases the proportion of β S450L-type Rifampicin-resistant mutants. AAP-SO2 acts synergistically with Rifampicin to kill non-replicating Mtb in a rabbit caseous necrosis model. AAP-SO2 can be used for the research of tuberculosis .
Cat. No.: HY-187361
CAS No.: 3107740-33-7
PROTAC HIV-1 degrader-1 is a HIV-1 capsid (CA) PROTAC degrader, with a DC50 of 3 nM against HIV-1IIIB (MT‑4 cells) and a DC50 of 1.17 nM against HIV-1NL4-3 (MT‑4 cells). PROTAC HIV-1 degrader-1 conjugates HIV-1 capsid (CA) with the VHL E3 ubiquitin ligase, triggering polyubiquitination and proteasome-mediated degradation of CA, as well as competitively inhibiting the binding of host factors CPSF6 and Sec24C to CA. PROTAC HIV-1 degrader-1 degrades CA drug-resistant mutants (N74D, K70R). PROTAC HIV-1 degrader-1 is applicable to research related to HIV-1 infection .
Cat. No.: HY-400902R
CAS No.: 2506273-81-8
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VT3989 (Standard) is the analytical standard of VT3989 (HY-400902). This product is intended for research and analytical applications. VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors .
Cat. No.: HY-E70700
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/T790M/C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/T790M/C797S/L858R protein that can be used to study EGFR d746-750/T790M/C797S/L858R-related functions .
NRX-0492 is an orally active BTK PROTAC degrader, with a binding IC50 of 1.2 nM for both wild-type BTK and BTK T474I, and 2.7 nM for BTK C481S, and exhibits cellular DC50 values of 0.1 nM and 0.2 nM against wild-type BTK and BTK C481S, respectively. NRX-0492 catalyzes the ubiquitination and proteasomal degradation of wild-type and drug-resistant mutant BTK by recruiting the CRBN E3 ubiquitin ligase complex. NRX-0492 inhibits the BCR signaling pathway and its downstream NF-κB/MYC transcriptional program, achieves rapid and sustained degradation in primary CLL cells, and exhibits extremely low cytotoxicity. NRX-0492 degrades BTK, inhibits tumor cell proliferation and activation, and significantly suppresses tumor growth in xenograft models. NRX-0492 can be used in research related to chronic lymphocytic leukemia and diffuse large B-cell lymphoma .
Cat. No.: HY-17539
CAS No.: 1421919-75-6
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KPT-276 is an orally active and blood-brain barrier-penetrant selective XPO1/CRM1 inhibitor. KPT-276 blocks XPO1-mediated nuclear export function and promotes nuclear retention of various tumor suppressor proteins. KPT-276 induces apoptosis and G1 cell cycle arrest in tumor cells, and downregulates c-MYC, CDC25A, and BRD4. KPT-276 reduces immune cell proliferation through nuclear accumulation of cell cycle inhibitors, rescues TDP-43 cytoplasmic mislocalization, and restores axon growth and growth rate in mutant PFN1 motor neurons. KPT-276 maintains axonal cytoskeletal integrity and mitochondrial function, and inhibits tumor growth. KPT-276 can be used for research on glioblastoma, non-Hodgkin lymphoma, amyotrophic lateral sclerosis, multiple myeloma, and non-small cell lung cancer .
Cat. No.: HY-179623
PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer .
Cat. No.: HY-183355
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KRAS G12D-IN-37 is a KRAS G12D inhibitor. KRAS G12D-IN-37 shows antiproliferative activity against KRAS G12D mutant tumor cells and minimal cytotoxicity toward normal cells. KRAS G12D-IN-37 binds stably to KRAS G12D via hydrogen bond interactions with residues His 95, Arg 68, and Asp 12, and inhibits downstream ERK/AKT signaling pathways. KRAS G12D-IN-37 elevates ROS levels, induces apoptosis, disrupts mitochondrial membrane potential. KRAS G12D-IN-37 downregulates the level of anti-apoptotic protein Bcl-2, and upregulates the levels of pro-apoptotic proteins Bax and caspase 3. KRAS G12D-IN-37 can be used for the research of cancer, such as gastric adenocarcinoma and colorectal cancer .
Cat. No.: HY-187629
CAS No.: 2202678-04-2
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HH2853 is an orally active EZH1/EZH2 inhibitor, with an IC50 of 9.26 nM for EZH1 and IC50 values ranging from 2.21 to 3.75 nM for both wild-type and mutant EZH2 . HH2853 simultaneously inhibits the methyltransferase activities of EZH1 and EZH2, blocks the compensatory pathway that arises following EZH2 inhibition, and reduces H3K27me3 levels. HH2853 upregulates the expression of c-Myc and TfR-1 to induce intracellular iron accumulation, and stabilizes GPX4 via HSPA5 to suppress ferroptosis. HH2853 combined with Erastin (HY-15763) synergistically inhibits EZH2 wild-type DLBCL cell proliferation. HH2853 alone shows weak activity against EZH2 wild-type DLBCL and is well tolerated. HH2853 is applicable for research related to diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, epithelioid sarcoma, and follicular lymphoma .
Cat. No.: HY-189210A
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TopBP1-IN-4 is a TopBP1 inhibitor, with an IC50 value of 2.47 to 3.8 nM against the TopBP1 BRCT7/8 domain. TopBP1-IN-4 selectively disrupts BRCT7/8-dependent oncogenic protein-protein interactions, does not interfere with other BRCT domain-mediated functions of TopBP1, and has no effect on DNA replication. TopBP1-IN-4 restores E2F1-mediated Apoptosis in cells. TopBP1-IN-4 induces mitotic catastrophe in cells. TopBP1-IN-4 overcomes Osimertinib (HY-15772) resistance in EGFR-mutant non-small cell lung cancer models. TopBP1-IN-4 can be used in studies related to triple-negative breast cancer, ovarian cancer, non-small cell lung cancer, and acute myeloid leukemia .
Cat. No.: HY-141878
CAS No.: 2767983-76-4
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di-Ellipticine-RIBOTAC is a RNase recruiting chimera (RIBOTAC) degrader, capable of specifically binding and degrading expanded G4C2 RNA repeat (r(G4C2) exp). di-Ellipticine-RIBOTAC selectively binds the three-dimensional (3D) structure formed by r(G4C2) exp and that recruits an endogenous ribonuclease (RNase) to cleave r(G4C2) exp. di-Ellipticine-RIBOTAC selectively degrades the mutant chromosome 9 open reading frame 72 (C9orf72) allele and reduces quantities of toxic dipeptide repeat proteins (DPRs) translated from r(G4C2) exp. di-Ellipticine-RIBOTAC significantly improves the pathological phenotype of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) in cells and mouse models. di-Ellipticine-RIBOTAC can be used for the study of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) .
Cat. No.: HY-178061
CAS No.: 2598870-24-5
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
Cat. No.: HY-180966
CAS No.: 3057939-66-6
Gly-PEG3-BA is an EML4-ALK PROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research .
Cat. No.: HY-188044
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DC-98-LC74 is a selective modulator of adult skeletal muscle-type nicotinic acetylcholine receptor (α1β1δε), with an EC50 value of 6.5 µM for the human receptor and an IC50 of 13.45 µM for the human α3β4 nicotinic acetylcholine receptor. DC-98-LC74 increases the ligand-free opening probability of the receptor via the ε subunit M2-M3 loop, and prolongs the burst duration and opening probability of wild-type and fast-channel mutant AChR. DC-98-LC74 exerts weak effects on neuronal AChR subtypes and has no agonist activity. DC-98-LC74 prolongs the mouse diaphragm endplate current and improves muscle contractility in isolated neuromuscular preparations from sarcopenic mice. DC-98-LC74 can be used for studies on neuromuscular junction function and myasthenia-related diseases .
Cat. No.: HY-12017C
CAS No.: 1159490-83-1
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PF-04217903 phosphate is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a Ki value of 4.8 nM and a Kd value of 4.5 nM. PF-04217903 phosphate blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 phosphate suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 phosphate retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 phosphate increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 phosphate is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis) .
Cat. No.: HY-13443S
Synonyms: Exenatide (Leu-13C6,15N) TFA
Exendin-4 (Leu- 13C6, 15N) TFA (Exenatide (Leu- 13C6, 15N) TFA) is the 13C, 15N-labeled Exendin-4 (HY-13443). Exendin‑4 (Exenatide) is an orally active, blood-brain barrier-permeable glucagon-like peptide-1 receptor (GLP‑1 receptor) agonist that resists degradation mediated by dipeptidyl peptidase IV. Exendin‑4 mediates multiple glucose-regulating effects, including stimulation of glucose-dependent insulin secretion, inhibition of glucagon production, increase in β-cell mass, delay of gastric emptying, reduction of food intake, improvement of peripheral insulin sensitivity, and restoration of normal islet structure. Exendin‑4 inhibits oxidative stress, alleviates inflammatory responses, and reduces neuronal apoptosis. Exendin‑4 reduces the aggregation level of mutant huntingtin, improves motor function, prolongs survival time, and regulates the expression levels of leptin and ghrelin. Exendin‑4 can be used in research related to type 2 diabetes, acute ischemic stroke, and Huntington's disease .
Cat. No.: HY-141878A
CAS No.: 2767983-77-5
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di-Ellipticine-RIBOTAC TFA is a RNase recruiting chimera (RIBOTAC) degrader, capable of specifically binding and degrading expanded G4C2 RNA repeat (r(G4C2) exp). di-Ellipticine-RIBOTAC TFA selectively binds the three-dimensional (3D) structure formed by r(G4C2) exp and that recruits an endogenous ribonuclease (RNase) to cleave r(G4C2) exp. di-Ellipticine-RIBOTAC TFA selectively degrades the mutant chromosome 9 open reading frame 72 (C9orf72) allele and reduces quantities of toxic dipeptide repeat proteins (DPRs) translated from r(G4C2) exp. di-Ellipticine-RIBOTAC TFA significantly improves the pathological phenotype of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) in cells and mouse models. di-Ellipticine-RIBOTAC TFA can be used for the study of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) .
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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
