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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
627 Results for "
esistant mutation
" in MedChemExpress (MCE) Product Catalog:
Products (627)
627 Results for "esistant mutation" in MCE Product Catalog:
Cat. No.: HY-181420A
CAS No.: 3029443-36-2
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BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
Cat. No.: HY-189129
RAS GTPase-IN-3 is a RAS GTPase inhibitor that targets multiple KRAS-Q61 mutant variants. RAS GTPase-IN-3 binds to the switch II pocket of GTP-bound KRAS-Q61R, positions its side-chain imidazole group near the GTP γ-phosphate, and accelerates GTP hydrolysis of KRAS-Q61. RAS GTPase-IN-3 inhibits Sos-catalyzed nucleotide exchange on GTP-bound KRAS. RAS GTPase-IN-3 only activates GTP hydrolysis of HRAS-Q61R/Q95H and NRAS-Q61R/L95H mutant proteins. RAS GTPase-IN-3 can be applied in research related to cancers driven by KRAS-Q61 mutations .
Cat. No.: HY-189146
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HDTAC EGFR Degrader-1 is an EGFR HDTAC (hypoxia-activated targeted protein degradation chimera) degrader with a DC50 of 1.76 μM. HDTAC EGFR Degrader-1 consists of a linker, a tumor hypoxia-activated group (HAG, a group that generates ROS under tumor hypoxic conditions), and an EGFR ligand. HDTAC EGFR Degrader-1 drives EGFR degradation through the proteasomal pathway. HDTAC EGFR Degrader-1 downregulates Caspase-3 under hypoxic conditions. HDTAC EGFR Degrader-1 can be used in research on non-small cell lung cancer harboring EGFR mutations (EGFR ligand: FAAH-IN-2 (HY-79511); HAG: Thalidomide-O-COOH (HY-103597); linker: NH2-PEG3 (HY-W007545)) .
Cat. No.: HY-E70305
CAS No.: 84012-69-1
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GlcNAc-1-Phosphotransferase is a Golgi membrane-bound glycosylphosphotransferase. GlcNAc-1-Phosphotransferase is composed of an α/β catalytic subunit encoded by the GNPTAB gene and a γ regulatory subunit encoded by the GNPTG gene, forming an α2β2γ2 hexameric complex. GlcNAc-1-Phosphotransferase catalyzes the transfer of GlcNAc-1-phosphate from UDP-GlcNAc to the C-6 hydroxyl group of terminal mannose residues on high-mannose-type N-glycans, thereby initiating the mannose-6-phosphate tagging pathway. GlcNAc-1-Phosphotransferase loss-of-function mutations can lead to lysosomal storage diseases such as mucolipidosis type II/III. GlcNAc-1-Phosphotransferase can be used in research related to mucolipidosis .
Cat. No.: HY-P990234
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Cat. No.: HY-P990235
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Cat. No.: HY-P99119A
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Infection Neurological Disease Inflammation/Immunology Cancer
Cat. No.: HY-P991839
Cat. No.: HY-L231
25 compounds
The TCA cycle (tricarboxylic acid cycle)—is also known as the Krebs cycle or the citric acid cycle (CAC). The TCA cycle is a series of chemical reactions that release stored energy through the oxidation of acetyl-CoA in carbohydrates, fats, and proteins.
For decades, the TCA cycle has been considered as the central pathway for cell oxidative phosphorylation to produce energy and biosynthesis. Research shows that TCA cycle is associated with many diseases, especially cancer. In colon carcinoma, liver cancer and other cancers, there are mutations that lead to the imbalance of TCA cycle metabolites, indicating that TCA cycle may be related to the occurrence of cancer. Understanding the role and molecular mechanism of TCA cycle in inhibiting or promoting cancer progression will promote the development of new metabolite-based cancer treatment methods in the future.
MCE supplies a unique collection of 25 key intermediates of the TCA cycle, which can be utilized for TCA-related research and metabolomics identification studies.
Cat. No.: HY-L201
3,628 compounds
Cell proliferation, the increase in cell numbers resulting from cell division, is a complex and tightly regulated process. Cell proliferation is regulated by coordinated entry into the cell cycle, and changes in proliferation are closely linked to disease development. Evolutionary dynamics links tumor growth and progression with cell proliferation, cell death, and mutation rates. In addition, cell proliferation is central to degenerative diseases, the development of which is often accompanied by accelerated multiplication of cancer cells. Therefore, assays of cell proliferation levels are frequently used for laboratory research purposes and increasingly for clinical assessment of tumor aggressiveness and potentially to guide care. It has been shown that multiple key targets are collectively involved in regulating the process of cell proliferation, such as CDK, E2F, pRB, β-Catenin, and others.
MCE collects 3,628 compounds that target and regulate key targets of cell proliferation, which can be used in studies of cell proliferation mechanisms and drug discovery.
Cat. No.: HY-L004
3,522 compounds
DNA is prone to numerous forms of damage that can injure cells and impair fitness. Cells have developed an array of mechanisms to repair these injuries. Proliferating cells are especially vulnerable to DNA damage due to the added demands of cellular growth and division. Cell cycle checkpoints represent integral components of DNA repair that coordinate cooperation between the machinery of the cell cycle and several biochemical pathways that respond to damage and restore DNA structure. By delaying progression through the cell cycle, checkpoints provide more time for repair before the critical phases of DNA replication, when the genome is replicated, and of mitosis, when the genome is segregated. Loss or attenuation of checkpoint function may increase spontaneous and induced gene mutations and chromosomal aberrations by reducing the efficiency of DNA repair.
MCE owns a unique collection of 3,522 cell cycle/DNA damage-related compounds which can be used in the research of the same.
Cat. No.: HY-L148
72 compounds
The TCA cycle (tricarboxylic acid cycle)—is also known as the Krebs cycle or the citric acid cycle (CAC). The TCA cycle is a series of chemical reactions that release stored energy through the oxidation of acetyl-CoA in carbohydrates, fats, and proteins.
For decades, the TCA cycle has been considered as the central pathway for cell oxidative phosphorylation to produce energy and biosynthesis. Research shows that TCA cycle is associated with many diseases, especially cancer. In colon carcinoma, liver cancer and other cancers, there are mutations that lead to the imbalance of TCA cycle metabolites, indicating that TCA cycle may be related to the occurrence of cancer. Understanding the role and molecular mechanism of TCA cycle in inhibiting or promoting cancer progression will promote the development of new metabolite-based cancer treatment methods in the future.
MCE supplies a unique collection of 72 compounds related to the TCA cycle. MCE TCA Cycle Compound Library is a useful tool for the TCA cycle related research and anti-cancer drug development.
Cat. No.: HY-134813R
CAS No.: 2621928-55-8
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MRTX1133 (Standard) is the analytical standard of MRTX1133 (HY-134813). This product is intended for research and analytical applications. MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
Cat. No.: HY-139997
CAS No.: 2140806-84-2
DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .
Cat. No.: HY-144657
CAS No.: 2913176-81-3
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(4S)-PROTAC SOS1 degrader-1 is a stereoisomer of PROTAC SOS1 degrader-1 (HY-145737). PROTAC SOS1 degrader-1 (Compound 9d) is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers .
Cat. No.: HY-144657A
Purity: 98.09%
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(4S)-PROTAC SOS1 degrader-1 diTFA is a stereoisomer of PROTAC SOS1 degrader-1 (HY-145737). PROTAC SOS1 degrader-1 (Compound 9d) is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers .
Cat. No.: HY-175529
KRASG12D-IN-7 is a selective KRAS G12D inhibitor. KRASG12D-IN-7 displays strong binding activity for KRAS G12D in both its GDP- and GTP- bound states, with Kd value of 1.12 nM and 1.86 nM, respectively. KRASG12D-IN-7 inhibits the proliferation of KRAS G12D harboring AsPC-1 cells with an IC50 value of 10 nM and suppresses MAPK signaling. KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis in AsPC-1 cells, and strongly inhibits their colony formation. KRASG12D-IN-7 can be used for the study of cancers harboring KRAS G12D mutation, particularly pancreatic ductal adenocarcinoma (PDAC) .
Cat. No.: HY-175864
EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR 19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .
Cat. No.: HY-178057
CAS No.: 2754394-10-8
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EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .
Cat. No.: HY-182044
MRTX849-amide-C4-(o)-carborane is a KRAS G12C inhibitor with mutation selectivity for cells expressing KRAS G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS G12C-positive cancers .
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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
