2′-O,4′-C-Methyleneguanosine (LNA-G) is a reverse guanine analogue, where LNA (locked nucleic acid) is a nucleic acid analogue. LNA modification can be used in a variety of applications such as effective binding affinity to complementary sequences and greater nuclease resistance than natural nucleotides, offering great potential for applications in disease diagnosis and research. LNA-G is also available via KOD DNA polymerase, which allows the integration of LNA-G nucleotides into the DNA strand[1][2].
Dapagliflozin (BMS-512148) is a sodium-glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
N-Methyl-dosimertinib-d5 is the deuterium labeled of Dosimertinib (HY-142283). Dosimertinib is a highly potent, selective, and orally active deuterated EGFR inhibiotor. Dosimertinib can be used for the research of non-small-cell lung cancer[1][2].
Fmoc-NH-PEG1-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
m-PEG7-CH2-OH a PEG-based based PROTAC linker can be used in the synthesis of PROTACs.
Tetraethyl decane-1,10-diylbis(phosphonate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Emtricitabine Degradant-III is a major degradation product of Emtricitabine. Emtricitabine is a potent nucleoside reverse transcriptase inhibitor used for the treatment of HIV infection.
Decursidate is an active compound. Decursidate can prolong thrombin time[1].
Tristin is a bibenzyl derivatives. Tristin is a nature product isolated from Dendrobii Herba (stems of Dendrobium spp.). Tristin has antioxidative activity[1].
Bis-(m-PEG8-amido)-hexanoic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway[1][2]. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
Sulfo-NHS-Acetate sodium is an alkyl chain-based PROTAC linker. Sulfo-NHS-Acetate sodium can be used in the synthesis of PROTACs[1].
Boc-(R)-3-thienylglycine is a Glycine (HY-Y0966) derivative[1].
Sodium hexadecyl sulfate-d33 is the deuterium labeled Sodium hexadecyl sulfate[1].
2,7-Bis(alloxycarbonylamino)-9-chloroacridine can be used as a fluorescent label.
endo-BCN-PEG3-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Fenbufen-d9 (CL-82204-d9) is the deuterium labeled Fenbufen. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor[1][2][3][4][5].
Boc-D-Trp(For)-OH, containing the amino acid tryptophan, is synthesized by the ammonolysis of Boc-protected D-alanine, followed by cyclization to form a dipeptide with ninhydrin. Boc-D-Trp(For)-OH has pharmacological properties, including inhibition of growth hormone release, induction of sleep and antiinflammatory[1][2].
meso-CF3-BODIPY 2 (CF3-substituted Tetramethyl BODIPY) is a fluorescent dye with the absorption wavelength (λabs) of 553 nm and emission wavelength (λem) of 622 nm. meso-CF3-BODIPY 2 can be used in labeling reagents and photodynamic therapy[1][2].
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research[1][2].
GP1a is a potent agonist of cannabinoid receptor 2 (CB2). Gp1a is beneficial to skin wound healing. GP1a inhibits inflammation and fibrogenesis while promoting re-epithelialization[1].
Syk-IN-1 (compound 4) is a potent Syk inhibitor, with an IC50 of 35 nM[1].
Anticancer agent 103 (Compound 2k) is a potent anticancer agent[1].
Boc-C16-COOH is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Boc-C16-COOH is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]
Ezetimibe-d4 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
HJB97 is a high-affinity BET inhibitor with Kis of 0.9±0.2 nM (BRD2 BD1), 0.27±0.09 nM (BRD2 BD2), 0.18±0.01 nM (BRD3 BD1), 0.21±0.03 nM (BRD3 BD2), 0.5±0.2 nM (BRD4 BD1), 1.0±0.1 nM (BRD4 BD2), respectively. HJB97 is a PROTAC BET degrader. Antitumor activity[1].
Azido-PEG5-CH2CO2-PFP is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs[1].
Ethylenediaminetetraacetic acid (EDTA) disodium dihydrate is a chelating agent used as a protease inhibitor and metal ion scavenger. Ethylenediaminetetraacetic acid disodium dihydrate is used extensively during protein purification. Ethylenediaminetetraacetic acid disodium dihydrate has been shown to be a noneffective molecule on cellulase activity. Ethylenediaminetetraacetic acid disodium dihydrate binds to metals including calcium and facilitates their excretion[1][2].
APS-2-79 behaves as a kinase suppressor of Ras (KSR)-dependent antagonist of RAF-mediated MEK phosphorylation. APS-2-79 binds directly to KSR2 within the KSR2-MEK1 complex with an IC 50 of 120±23 nM for KSR2.