9月
Gersizangitide；GersizangitideGersizangitide (2024/9/8)
簡(jiǎn)介：gersizangitide is an angiogenesis inhibitor.
PROTAC BRD4 Degrader-13；PROTAC BRD4 Degrader-13PROTAC BRD4 Degrader-13；PROTAC BRD4 Degrader-13 (2024/9/8)
簡(jiǎn)介：protac brd4 degrader-13 (compound 9d) is a bioactive compound that functions as a proteolysis targeting chimera (protac), linking ligands for von hippel-lindau and brd4 proteins. in the context of pc3 prostate cancer cells, this compound effectively degrades the brd4 protein through conjugation with steap1 and cll1 antibodies. the degradation of brd4 protein is achieved with remarkable potency, exhibiting a dc 50 of 0.025 nm and 6.0 nm when combined with steap1 and cll1 antibodies, respectively.
PROTAC BRD4 Degrader-15；PROTAC BRD4 Degrader-15PROTAC BRD4 Degrader-15；PROTAC BRD4 Degrader-15 (2024/9/8)
簡(jiǎn)介：protac brd4 degrader-15 is a chemical compound consisting of a proteolysis targeting chimera (protac) linked to ligands specific to von hippel-lindau and brd4. it exhibits an ic50 of 7.2 nm for brd4 bd1 and 8.1 nm for brd4 bd2. additionally, protac brd4 degrader-15 demonstrates potent degradation activity against the brd4 protein in pc3 prostate cancer cells.
PROTAC BRD4 Degrader-10；PROTAC BRD4 Degrader-10PROTAC BRD4 Degrader-10；PROTAC BRD4 Degrader-10 (2024/9/8)
簡(jiǎn)介：protac brd4 degrader-10, also known as compound 8b, is a dual ligand-based protac that combines ligands for von hippel-lindau and brd4. to degrade the brd4 protein in pc3 prostate cancer cells, protac brd4 degrader-10 can be conjugated with steap1 and cll1 antibodies, with respective dc 50 values of 1.3 nm and 18 nm.
PROTAC BRD4 Degrader-9；PROTAC BRD4 Degrader-9PROTAC BRD4 Degrader-9；PROTAC BRD4 Degrader-9 (2024/9/8)
簡(jiǎn)介：protac brd4 degrader-9 (compound 8a) is a novel chemical compound consisting of ligands for von hippel-lindau and brd4, connected by a protac moiety. this compound can effectively degrade the brd4 protein in pc3 prostate cancer cells. when conjugated with steap1 and cll1 antibodies, protac brd4 degrader-9 exhibits potent activity, with respective dc50 values of 0.86 nm and 7.6 nm.
Cavα2δ-IN-1；Cavα2δ-IN-1Cavα2δ-IN-1 (2024/9/8)
簡(jiǎn)介：cavα2δ-in-1 demonstrates exceptional specificity for voltage-gated calcium channels cavα2δ-1 (with a ki value of 6 nm), in comparison to cavα2δ-2 (with a ki value greater than 10,000 nm).
S65487 sulfateS65487 sulfateVOB560 sulfate (2024/9/8)
簡(jiǎn)介：s65487 (vob560) sulfate, a potent and selective bcl-2 inhibitor, demonstrates activity against bcl-2 mutations, including g101v and d103y. it exhibits poor affinity for mcl-1, bfl-1, and bcl-xl. additionally, s65487 sulfate induces apoptosis and possesses anticancer activities.
Eticlopride hydrochloride；依替必利鹽酸鹽Eticlopride hydrochloride (2024/9/8)
簡(jiǎn)介：eticlopride, an antipsychotic, is a selective dopamine d2/d3 receptor antagonist (ki: 0.5/0.16 nm).
SENP1-IN-2SENP1-IN-2SENP1-IN-2 (2024/9/8)
簡(jiǎn)介：senp1-in-2, a distinct inhibitor of the desumoylation protease 1 (senp1), is designed to enhance tumor radiosensitivity.
SENP1-IN-4SENP1-IN-4SENP1-IN-4 (2024/9/8)
簡(jiǎn)介：senp1-in-4, a distinct inhibitor of the desumoylation protease 1 (senp1), is designed to enhance tumor radiosensitivity.
SENP1-IN-3SENP1-IN-3SENP1-IN-3 (2024/9/8)
簡(jiǎn)介：senp1-in-3 is a distinct inhibitor of the desumoylation protease 1 (senp1), designed to enhance tumor radiosensitivity.
ALK2-IN-4 succinateALK2-IN-4 succinateALK2-IN-4 succinate (2024/9/8)
簡(jiǎn)介：alk2-in-4 succinate is a robust and effective inhibitor of alk2.
V-9302 hydrochloride；V-9302 hydrochlorideV-9302 hydrochloride (2024/9/8)
簡(jiǎn)介：v-9302 hydrochloride is a potent and selective competitive antagonist that inhibits transmembrane glutamine flux by specifically targeting the amino acid transporter asct2 (slc1a5), and not asct1. in hek-293 cells, v-9302 hydrochloride effectively inhibits asct2-mediated glutamine uptake with an ic50 value of 9.6 μm.
CBR-470-1；化合物CBR-470-1CBR-470-1 (2024/9/8)
簡(jiǎn)介：cbr-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (pgk1) that activates nrf2 by increasing methylglyoxal levels. cbr-470-1 is a non-covalent nrf2 activator with neuroprotective activity that protects sh-sy5y neuronal cells from mpp+-induced cytotoxicity by activating the keap1-nrf2 cascade. cytotoxicity induced by mpp+.
DDR1-IN-5；DDR1-IN-5DDR1-IN-5；DDR1-IN-5 (2024/9/8)
簡(jiǎn)介：ddr1-in-5 is a potent and selective inhibitor of the discoidin domain receptor family, member 1 (ddr1). it effectively inhibits the phosphorylation of ddr1b (y513) with an ic 50 value of 4.1 nm. furthermore, ddr1-in-5 demonstrates remarkable anti-cancer activity. its inhibitory potency against ddr1 (ic 50 = 7.36 nm) makes it a promising compound for targeted therapy in cancer treatment.
DDR1-IN-6；DDR1-IN-6DDR1-IN-6；DDR1-IN-6 (2024/9/8)
簡(jiǎn)介：ddr1-in-6 is a potent and selective inhibitor of discoidin domain receptor family member 1 (ddr1), exhibiting remarkable inhibitory activity at an ic50 of 9.72 nm. it effectively suppresses the auto-phosphorylation of ddr1b (y513) with an ic50 value of 9.7 nm. furthermore, ddr1-in-6 displays strong anti-cancer activity.
Nicotinamide riboside malate；煙酰胺核糖蘋果酸鹽Nicotinamide riboside malate (2024/9/8)
簡(jiǎn)介：nicotinamide riboside malate is an orally active nad+ precursor that elevates nad+ levels and stimulates the activity of sirt1 and sirt3. functioning as a vitamin b3 (niacin) source, it augments oxidative metabolism and provides protection against metabolic abnormalities induced by a high-fat diet. additionally, nicotinamide riboside malate mitigates cognitive decline in a genetically modified mouse model of alzheimer´s disease.
Pentostatin；噴司他丁Nipent|||CI-825|||Covidarabine|||Deoxycoformycin；Nipent|||CI-825|||Covidarabine|||噴司 (2024/9/8)
簡(jiǎn)介：pentostatin (ci-825) is an extremely effective and irreversible inhibitor of adenosine deaminase (ki: 2.5 pm).
Nicotinamide riboside tartrate；煙酰胺核糖酒石酸鹽Nicotinamide riboside tartrate (2024/9/8)
簡(jiǎn)介：nicotinamide riboside tartrate (nrt) is an oral nad+ precursor that raises nad+ levels, activates sirt1 and sirt3, and serves as a vitamin b3 (niacin) source. nrt also improves oxidative metabolism and protects against metabolic abnormalities induced by a high-fat diet. furthermore, nrt mitigates cognitive decline in a transgenic mouse model of alzheimer´s disease.
IQZ23；IQZ23IQZ23；IQZ23 (2024/9/8)
簡(jiǎn)介：iqz23 is a chemical compound that effectively inhibits adipocyte differentiation by activating the ampk pathway. it demonstrates high efficacy in reducing triglyceride levels (ec50=0.033 μm) in 3t3-l1 adipocytes. given its properties, iqz23 holds potential for research related to obesity and metabolic disorders.
HJC0416 hydrochloride；HJC0416 hydrochlorideHJC0416 hydrochloride (2024/9/8)
簡(jiǎn)介：hjc0416 hydrochloride, a potent, orally active inhibitor of stat3, exhibits a superior anticancer profile compared to stattic. it stands out as a promising agent for breast cancer research.
TP-238 hydrochloride；TP-238 hydrochlorideTP-238 hydrochloride (2024/9/8)
簡(jiǎn)介：tp-238 hydrochloride is a highly potent and selective dual cecr2/bptf probe, demonstrating ic50 values of 30 nm and 350 nm, respectively. it additionally exerts inhibitory effects on brd9, with a pic50 value of 5.9, while displaying lower activity against 338 other kinases.
A 410099.1 amide-PEG3-amine-Boc；A 410099.1 amide-PEG3-amine-BocA 410099.1 amide-PEG3-amine-Boc；A 410 (2024/9/8)
簡(jiǎn)介：a 410099.1 amide-peg3-amine-boc is an iap ligand-based functionalized molecule commonly used in protacs. it comprises an iap ligand and an amide-peg3 linker that possesses a terminal amine. the compound can successfully conjugate with target protein ligands.
Boc-A 410099.1 amide-alkylC4-amine；Boc-A 410099.1 amide-alkylC4-amineBoc-A 410099.1 amide-alkylC4-am (2024/9/8)
簡(jiǎn)介：boc-a 410099.1 amide-alkylc4-amine is a functionalized iap ligand for protacs, comprising of an iap ligand and an amide-alkylc4 linker terminating in an amine group. it has the ability to form conjugates with target protein ligands.
A 410099.1 amide-PEG2-amine-Boc；A 410099.1 amide-PEG2-amine-BocA 410099.1 amide-PEG2-amine-Boc；A 410 (2024/9/8)
簡(jiǎn)介：a 410099.1 amide-peg2-amine-boc is a functionalized iap ligand for protacs, consisting of an iap ligand and an amide-peg3 linker with a terminal amine. it is capable of forming conjugates with target protein ligands.
Acid Ceramidase-IN-1；Acid Ceramidase-IN-1Acid Ceramidase-IN-1 (2024/9/8)
簡(jiǎn)介：acid ceramidase-in-1 is a highly effective and orally bioavailable inhibitor of acid ceramidase (ac, asah-1), with an inhibitory concentration (ic50) of 0.166 μm. additionally, acid ceramidase-in-1 exhibits exceptional brain penetration capabilities in mice.
FDI-6；化合物FDI6FDI6|||FDI 6；FDI6|||FDI 6 (2024/9/8)
簡(jiǎn)介：fdi-6 is an effective and selective inhibitor of foxm1 that blocks dna binding. fdi-6(fdi6) binds to the foxm1 protein and specifically downregulates foxm1-activated genes.
MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin；MC-AAA-NHCH2OCH2COO-7-aminomethyl (2024/9/8)
簡(jiǎn)介：mc-aaa-nhch2och2coo-7-aminomethyl-10-methyl-11-fluoro camptothecin (compound 21a), is a camptothecin payload which can be utilized in the synthesis of a camptothecin antibody-drug conjugate (adc) by conjugation to a monoclonal antibody (mab).
MC-AAA-NHCH2OCH2COOH；MC-AAA-NHCH2OCH2COOHMC-AAA-NHCH2OCH2COOH；MC-AAA-NHCH2OCH2COOH (2024/9/8)
簡(jiǎn)介：mc-aaa-nhch2och2cooh (compound 20) is a cleavable antibody-drug conjugate (adc) linker. its primary application lies in the synthesis of adcs.
CDK6/9-IN-1CDK6/9-IN-1CDK6/9-IN-1 (2024/9/8)
簡(jiǎn)介：cdk6/9-in-1 (compound 66) is a potent dual inhibitor of cdk 6 and cdk 9 that can be administered orally. it exhibits inhibitory activity with ic 50 values of 40.5 nm and 39.5 nm against cdk6 and cdk9, respectively.
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