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.

Clorgyline hydrochloride (M&B 9302 hydrochloride) is a selective, irreversible monoamine oxidase A (MAO-A) inhibitor that can cross the blood-brain barrier and exhibits activity against the 5-HT Receptor at very high doses. Clorgyline hydrochloride regulates monoamine neurotransmitter levels, the release of dopamine and acetylcholine, the uptake and effects of Tyramine (HY-W007606), noradrenergic function, circadian locomotor activity rhythms, feeding behavior, and body weight. Clorgyline hydrochloride induces tumor-suppressive transcriptional programs, secretory differentiation, androgen signaling regulation, Bcl-2 expression, and radioprotective effects in non-malignant cells. Clorgyline hydrochloride is used in the research of high-grade prostate cancer, Huntington's disease, major affective disorder, radiation-induced normal tissue toxicity, and obesity.

Oleic acid alkyne is Oleic acid (HY-N1446) with an acetylene group. The terminal alkyne group can be used for click chemical ligation reactions. Oleic acid can be hydroxylated by a microsomal cytochrome P-450-dependent system (ω-OAH). Through click chemistry reactions, fluorescent or biotin-labeled oleic acid can be introduced to analyze its metabolism and biological activity.

MCB-36 is a pan-KRAS PROTAC degrader that recruits VHL, with a K_d value of approximately 1 pM against KRAS, and it does not affect KRAS transcription. MCB-36 continuously degrades various KRAS mutants, inhibits oncogenic KRAS signaling pathways, reduces p-ERK levels, and induces apoptosis, thereby suppressing the growth of KRAS-dependent cancer cells. In vivo, MCB-36 inhibits tumor growth, overcomes resistance to KRAS G12C inhibitors, remodels the tumor immune microenvironment and enhances immune cell infiltration. MCB-36 can be used in research related to colorectal cancer and lung cancer.

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.

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.

IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection. IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling. IA-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.