Poncirin is isolated from Poncirus trifoliata with anti-inflammory activites. Poncirin significantly reduces mechanical hyperalgesia and allodynia in Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models[1].
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity[1][2].
t-Boc-Aminooxy-PEG7-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Palmitic acid-9,10-d2 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
Atazanavir(BMS-232632) is an highly potent HIV-1 protease inhibitor.IC50 value:Target: HIV-1 protease inhibitorAtazanavir sulfate is a sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor. It has a pharmacokinetic profile that supports once-daily dosing and has demonstrated a unique resistance profile and superior virologic potency compared with other antiretrovirals in vitro. In subjects with HIV, atazanavir (400 mg once daily) produced rapid and sustained improvements in viral load and CD4 counts in both antiretroviral-naive as well as previously treated patients when used in combination with dual nucleoside reverse transcriptase inhibitor (NRTI) treatment [1].After intravenous (iv), oral (po) and intraportal (ip) administration of ATV at a dosage of 7 mg/kg, AUCs in HL rats were 12.41, 5.24 and 8.89 microg/mLh, respectively, and were significantly higher than those in control rats (4.09, 1.70 and 3.38 microg/mLh). Despite the decrease of distribution volume (Vd(ss)), the terminal half-life (t(1/2)) in HL tended to be shorter than in control, and hepatic distribution of ATV in HL rats was 4.8-fold increases. These results suggested that the uptake of ATV into liver might counteract the decrease of Vd(ss). On the other hand, there was no significant difference in bioavailability, and the lymphatic transport to AUC showed no statistical change. In conclusion, although the protein binding rate and AUC were significantly increased, the pharmacokinetics of ATV might be tolerated in HL [2].Clinical indications: HIV-1 infection Toxicity: torsades de pointes
Rutin, a naturally occurring flavonoid glycoside, has antioxidant, anti-inflammatory, anti-allergic, anti-angiogenic and antiviral properties.
1,4-PBIT (1,4-PB-ITU) dihydrobromide (compound 46) is a potent nitric oxide synthases (NOS) inhibitor, with Ki values of 7.6 nM, 360 nM, and 16 nM for the inducible (iNOS), endothelial (eNOS), and neuronal (nNOS) isozymes, respectively[1].
Pelitinib-d6 (EKB-569-d6) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively[1][2].
PROTAC PTPN2 degrader-2 (example 187B) TFA is a potent PTPN2 degrader with potential for studying cancer or metabolic diseases[1].
Spiramine A (Spiramine C acetate (ester)) is a diterpene alkaloid with antitumor and antimicrobial activity. Spiramine A inhibits PAF-induced rabbit platelet aggregation in a concentration-dependent manner, with an IC50 vallue of 6.7 μM[1].
Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities[1][2][3].
KRAS G12C inhibitor 50 (Example 4) is a KRAS G12C inhibitor with an IC50 of 46.7 nM[1].
m-PEG9-SH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Monoethyl fumarate is the monoethyl ester form of fumaric acid. Monoethyl fumarate is a kind of effective preservative and polymerization agent for macromolecular material[1].
Serinol-d5 is the deuterium labeled Serino[1].
RASP-IN-1 (compound A) is a lipophili ccompound used for macular degeneration inhibition. RASP-IN-1 is biologically active in the retina of the rabbit's eye. Thirty minutes after IP treatment with 14C-RASP-IN-1 (10 mg/kg)，the Cmax amount of 14C-RASP-IN-1 in the posterior eye cup is 14.36 μg/g in mice model[1].
DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM)[1].
6-Amino-1,2-dihydro-2-β-D-ribofuranosyl-4H-pyrazolo[3,4-d]pyrimidin-4-one is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Anakinra is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Anakinra is the first biological agent to block the pro-inflammatory effects[1][2].
4-Nitro-DL-phenylalanine Hydrate is a phenylalanine derivative[1].
AIMP2-DX2-IN-1 (Compound 35) is a potent AIMP2-DX2 inhibitor with an IC50 of 0.1063 μM[1].
Dermaseptin, a peptide isolated from frog skin, exhibits potent antimicrobial activity against bacteria, fungi and protozoa.
Dexchlorpheniramine is an potent and blood-brain barrier (BBB) penetrant histamine 1 (H1) receptor antagonist with anticholinergic properties. Dexchlorpheniramine can be used for researching allergies[1].
PROTAC Linker 26 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 26 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Betahistine Dihydrochloride is a histamine H3 receptors inhibitor used as an antivertigo drug.Target: Histamine ReceptorBetahistine, a structural analogue of histamine with weak histamine H(1) receptor agonist and more potent H(3) receptor antagonist properties. Betahistine acts centrally by enhancing histamine synthesis within tuberomammillary nuclei of the posterior hypothalamus and histamine release within vestibular nuclei through antagonism of H(3) autoreceptors [1].Therapeutic effects of betahistine in vestibular disorders result from its antagonist properties at histamine H(3) receptors (H(3)Rs). On inhibition of cAMP formation and [(3)H]arachidonic acid release, betahistine behaved as a nanomolar inverse agonist and a micromolar agonist. After acute oral administration, Betahistine increased t-MeHA levels with an ED(50) of 2 mg/kg, a rightward shift probably caused by almost complete first-pass metabolism. Therapeutic effects of betahistine result from an enhancement of histamine neuron activity induced by inverse agonism at H(3) autoreceptors [2].
2-Aminopurine dihydrochloride is a fluorescent analog of guanosine. 2-Aminopurine dihydrochloride can be used as a fluorescence probe for nucleic acid structure and dynamics. Incorporating 2-Aminopurine dihydrochloride into DNA quenches its fluorescence[1][2].
Diethylamine-d6-hydrochloride is the deuterium labeled Diethylamine hydrochloride[1].
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6,6′-Dithiodinicotinic acid is a sulfur-containing organic compound belonging to nicotinic acid derivatives, which can be used as a specific sulfhydryl blocker[1].
Dalotuzumab (MK-0646) is a recombinant humanized monoclonal antibody (IgG1 type) targeting IGF-1R. Dalotuzumab acts by inhibiting IGF-1- and IGF-2-mediated tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation. Dalotuzumab also induces Apoptosis and cycle arrest. Dalotuzumab in combination with other anticancer drugs such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo[1][2][3].