6-Methoxytricin (Compound 6) is an flavonoid isolated from Artemisia iwayomogi. 6-Methoxytricin (Compound 6) is an inhibitor on aldose reductase (AR) and advanced glycation endproduct (AGE) formation activities with IC50 values of 30.29 μM and 134.88 μM, respectively. 6-Methoxytricin (Compound 6) has potential as an anti-diabetic complications agent[1].
Mitapivat is a potent human R-type pyruvate kinase (PKR) inhibitor; also shows potency for mutant PKR including R510Q PKR, R532W PKR, T384W PKR etc.
Dibucaine Hydrochloride is a local anesthetic of the amide type now generally used for surface anesthesia.Target: Sodium ChannelDibucaine is an amide local anesthetic. Dibucaine reduced the degradation of BSA-gold complex in the reservosomes, which was not caused either by an inhibition of the whole proteolytic activity of the parasite or by a reduction on the expression levels of cruzipain [1].Dibucaine, a quaternary ammonium compound, inhibited SChE to a minimum within 2 min in a reversible manner. The inhibition was very potent. It had an IC(50) of 5.3 microM with BuTch or 3.8 microM with AcTch. The inhibition was competitive with respect to BuTch with a K(i) of 1.3 microM and a linear-mixed type (competitive/noncompetitive) with respect to AcTch with inhibition constants, K(i) and K(I) of 0.66 and 2.5 microM, respectively. Dibucaine possesses a butoxy side chain that is similar to the butryl group of BuTch and longer by an ethylene group from AcTch [2].
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1[1].
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors[1].
Fibrinogen-Binding Peptide (designed by anticomplementarity hypothesis) is a presumptive peptide mimic of the vitronectin binding site on the fibrinogen receptor. Fibrinogen-Binding Peptide binds fibrinogen and inhibits both the adhesion of platelets to fibrinogen and platelet aggregation, and also inhibits the adhesion of platelets to vitronectin[1].
Dihydrotamarixetin (4'-O-Methyldihydroquercetin; Blumeatin A) is a flavonoid with the saturated 2,3-bond. Flavonoids with the saturated 2,3-bond are more powerful than unsaturated compounds[1].
JAK2 JH2 Tracer is a fluorescent probe for the JAK2 JH2 domain, with Kd of 0.2 μM.
Verapamil hydrochloride is a calcium channel antagonist.
DL-Cystathionine is a mixture of 4 isomers of cystathionine and allocystathionine, also is an intermediate in the biosynthesis of amino acid cysteine [1].
Noscapine is an orally administrable drug used worldwide for cough suppression, primarily mediated by its σ-receptor agonist activity, and possess anticancer activity.Target: σ-receptorin vitro: Noscapine is a phthalideisoquinoline alkaloid from opium, is a recently discovered anticancer drug and is currently under investigation in phase-I/II clinical trials for the treatment of leukemia and lymphoma. Noscapine causes few or no side effects and has been widely used as a cough suppressant in developing countries. Noscapine has been demonstrated to interact with microtubules. Interestingly, unlike many other microtubule-targeting agents such as Paclitaxel and Nocodazole, Noscapine does not obviously affect the total amount of microtubule polymers in cells; instead, it significantly increases the time microtubules spend in the pause state. The alteration of microtubule dynamics then activates the spindle checkpoint and arrests cell cycle progression at mitosis, leading to apoptotic cell death.
ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
A highly potent, selective inhibitor of checkpoint kinase TTK/Mps1 with IC50 of 0.6 nM; displays >200-fold selectivity over 276 kinases, including Aurora C, PLK1, PLK4; shows very potent anti-proliferative activity on a broad panel of human cancer cell lines (IC50=18- 897 nM); increases the survival in a murine breast cancer model that mimics human TNBC and delays tumor relapse, combined with docetaxel.
PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
Ala-Ala-βNA is a dipeptidyl-fl-naphthylamide (βNA). Ala-Ala-βNA is readily hydrolyzed, with optimum hydrolysis pH of 8.5-9.0[1].
Purine-9-b-D-(3’,5’-di-O-benzoyl-2’-deoxy-2’-fluoro)arabinoriboside is a purine nucleoside analog. 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].
Baohuoside VII is a flavonoid isolated from Herba Epimedii, with anti-osteoporosis activities[1].
4-Pentynoic acid (Propargylacetic acid) is an intermediate to produce biologically active compounds. 4-Pentynoic acid is widely utilized as a building block for the synthesis of eight sequence-defined model oligomers[1].
Daunorubicin is a topoisomerase II inhibitor.
Heptadecan-9-yl 8-bromooctanoate can be useful for the building or modification of lipid nanoparticles.
PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor.
FAM-dT phosphoramidite (Compound 21) is a fully protected labelled nucleoside phosphoramidite that can be incorporated into oligonucleotides[1].
H-D-Gly(allyl)-OH is a Glycine (HY-Y0966) derivative[1].
Aurachin SS is a nature product that could be isolated from Streptomyces sp. NA04227. Aurachin SS is an antibiotic and has antibacterial activity[1].
Fabimycin is a FabI inhibitor with potent antibacterial activity against gram-negative bacteria. Fabimycin is effective against drug-resistant gram-negative Infections in vivo[1].
Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice[1].
rac-Boc-β2-homophenylalanine is a phenylalanine derivative[1].
LM22A-4 is a specific agonist of tyrosine kinase receptor B, used for neurological disease research.
ANT3310 sodium is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). ANT3310 sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). ANT3310 sodium can be used in the research of bacterial infection[1][2].
REA is a peptide. REA recognizes lymphatics of a premalignant stage, but not to the tumor lymphatic vessels[1].