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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
595 Results for "
SCO2 mutations
" in MedChemExpress (MCE) Product Catalog:
Products (595)
595 Results for "SCO2 mutations" in MCE Product Catalog:
Cat. No.: HY-163679
Research Areas:
PROTAC ERα Degrader-9 is a dual-target degrader of estrogen receptor α (ERα) and aromatase (ARO/CYP19A), with a Ki value of 0.25 μM against human ERα and an IC50 value of 4.6 μM against human ARO. PROTAC ERα Degrader-9 degrades ERα and ARO via the ubiquitin-proteasome system, and inhibits the transcriptional activity of ERα and the enzymatic activity of ARO. PROTAC ERα Degrader-9 selectively inhibits cancer cell proliferation, induces cell cycle arrest, and triggers apoptosis. PROTAC ERα Degrader-9 exhibits antiproliferative activity and ERα-degrading activity against cancer cells carrying ERα mutations. PROTAC ERα Degrader-9 can be used in cancer-related research such as breast cancer .
Cat. No.: HY-170928
CAS No.: 2756978-82-0
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DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .
Cat. No.: HY-172877
Target:
Research Areas:
EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway .
Cat. No.: HY-178786
CAS No.: 2491726-04-4
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RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC50s: 1.4 nM, 1.9 nM, 3.8 nM for RET WT, RET V804L, RET V804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC50s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers .
Cat. No.: HY-178938
CAS No.: 1182011-65-9
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AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC) .
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 [2].
Cat. No.: HY-185899A
Synonyms: 5-Aza-2'-deoxycytidine-5′-triphosphate tetraTEA
5-Aza-dCTP tetraTEA (5-Aza-2'-deoxycytidine-5′-triphosphate tetraTEA) is a nucleotide analog that acts as a substrate for mammalian DNA polymerase α (Km = 3.0 μM) and a weak competitive inhibitor of this enzyme (Ki = 4.3 μM). 5-Aza-dCTP tetraTEA inhibits DNA polymerase α via incorporation into DNA through Watson-Crick base pairing, inhibits DNA methyltransferases via incorporation into hemimethylated DNA, and induces mutations in HIV-1 via incorporation into viral DNA during synthesis. 5-Aza-dCTP tetraTEA reverses the inhibitory effect of dTTP on dCMP deaminase, and allosterically activates dCMP deamination to the same extent as dCTP. 5-Aza-dCTP tetraTEA is applicable to research related to leukemia and type 1 human immunodeficiency virus infection [2] .
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
Research Areas:
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 [2] .
Cat. No.: HY-P990234
Target:
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Cat. No.: HY-P990235
Target:
Research Areas:
Cat. No.: HY-P99119A
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Cat. No.: HY-P991839
Cat. No.: HY-P99396A
Synonyms: MAB92 (LALA); BI 655130 (LALA)
Target:
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Spesolimab (MAB92; BI 655130) (LALA) is a humanized IgG1k antibody against IL-36R with a Kd value of 20 pM. Spesolimab (LALA) selectively blocks IL-36R signaling without inhibiting related interleukin pathways. Spesolimab (LALA) lacks functional cross-reactivity with non-human IL-36R and exhibits species-specific binding to human IL-36R, with reduced affinity for mouse, rat, hamster, minipig, and non-human primate IL-36R. Spesolimab (LALA) has L234A and L235A mutations introduced into the Fc region, designed to reduce antibody binding to FcγR and C1q, thereby attenuating/eliminating the ADCC and CDC effector functions of the antibody. Spesolimab (LALA) can be used for research on generalized pustular psoriasis (GPP) [2].
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
3,731 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 3,731 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
3,617 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 3,617 cell cycle/DNA damage-related compounds which can be used in the research of the same.
Cat. No.: HY-L148
73 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 73 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
Target:
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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 [2].
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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
