Alkynes

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 K_D 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.

5-Ethynyl-2'-deoxyuridine (EdU), a thymidine analogue, is incorporated into cellular DNA during DNA replication and the subsequent reaction of EdU with a fluorescent azide in a “Click” reaction. EdU staining is a fast, sensitive and reproducible method to study cell proliferation. 5-Ethynyl-2'-deoxyuridine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. 5-Ethynyl-2'-deoxyuridine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions.

O-Propargyl-Puromycin, an alkyne analog of puromycin, is a potent protein synthesis inhibitor. O-Propargyl-Puromycin is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

5-Ethynyluridine (5-EU) is a potent cell-permeable nucleoside can be used to label newly synthesized RNA. 5-Ethynyluridine can be used for isolation and sequencing of nascent RNA from neuronal populations in vivo. 5-Ethynyluridine can be used to identify changes in transcription in vivo in nervous system disease models. 5-Ethynyluridine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

GPX4-IN-1 is a potent GPX4 inhibitor. GPX4 shows antiproliferative activity. GPX4-IN-1 has the potential for the research of cancer.

PFI-3 Control is an inactive analog of PFI-3 (HY-12409), serving as an inactive negative control. PFI-3 Control shows no detectable binding activity toward purified PB1 (5), SMARCA2A, SMARCA2B, and SMARCA4 family VIII bromodomain proteins.

SW208108 is a prodrug of dMe-SW208108, a CYP4F11-activated SCD inhibitor, with an IC₅₀ value of 9 nM. SW208108 undergoes demethylation by CYP4F11 to form the active metabolite dMe-SW208108, thereby inhibiting enzyme function. SW208108 depletes unsaturated fatty acids, induces cytotoxicity in non-small cell lung cancer (NSCLC) cells expressing CYP4F11, and does not affect SCD activity in mouse sebocytes. SW208108 can be used in studies related to NSCLC.

Alkyne-phenol (Alk-Ph) is a clickable ascorbate peroxidase 2 (APEX2) probe. Alkyne-phenol substantially improves APEX-labeling efficiency in intact yeast cells, as it is more cell wall-permeant than APEX2 substrate biotin-phenol (BP). Alkyne-phenol also facilitates the identification of APEX-labeling sites, allowing the unambiguous assignment of membrane topology of mitochondrial proteins. Alkyne-phenol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a K_d of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions. EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Itaconate-alkyne (ITalk) is a specific bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of Itaconation in living cells. Itaconate-alkyne, a functional analogue of Itaconate, exhibits comparable antiinflammatory effect with Itaconate and enables the labeling of bona fide targets of Itaconate. Itaconate-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a K_i of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment. Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Alkynyl Palmitic Acid (Alk-C16) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. Alkynyl Palmitic Acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

L-β-ethynylserine (βES) is a threonine analog. L-β-ethynylserine is efficiently incorporated into newly synthesized proteins, and allows their selective visualization or enrichment through bioorthogonal ligation to fluorescent dyes or affinity tags, respectively.

Biotin alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Biotin alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Ethinylestradiol is an orally active steroidal estrogen. Ethinylestradiol is widely used in research on menopausal symptoms, gynecological conditions, and certain hormone-sensitive cancers.

L-Homopropargylglycine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. L-homopropargylglycine is an amino acid analog of methionine containing an alkyne moiety that can undergo a classic click chemical reaction with azide containing Alexa Fluor.

Clorgyline hydrochloride is an irreversible and selective inhibitor of monoamine oxidase A (MAO-A) that is used in scientific research, structurally related to Pargyline (HY-A0091A). Clorgyline hydrochloride has little effect on the amounts of conjugated dopamine (DA) present in superfusate of slices from rat striatum. Clorgyline hydrochloride contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.

DL-Propargylglycine is a Glycine (HY-Y0966) derivative. DL-Propargylglycine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.