BTK-IN-24 (compound 195) is a potent BTK inhibitor via a ubiquitin proteolytic pathway[1].
Precocene II is the insect antijuvenile hormone[1].
Anti-infective agent 2 (compound 3k) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.07 and 2.20 μM, respectively. Anti-infective agent 2 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 32 μg/mL[1].
DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.
TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].
Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic drugs[1].
LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with high affinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity[1][2].
Thalidomide-5-NH-CH2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-5-NH-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-NH-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
6-Diazo-5-oxo-D-norleucine is a leucine derivative[1].
APB is a cell-permeable, efficient kinase cosubstrate with conversions and kinetics similar to those of other known ATP analogues. APB shows a cytotoxicity EC50 value of 19 ± 1 mM.APB is shown to promote biotin labeling of kinase substrates in live cells and has future applications in phosphoprotein purification and analysis. APB is cell-permeable and nontoxic at low mM concentrations, with cell penetration and labeling dependent on the polyamine linker.
H-Thr(tBu)-OH is a threonine derivative[1].
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer[1][2].
Boc-L-Cys(Propargyl)-OH is a click chemistry reagent. Boc-L-Cys(Propargyl)-OH can be used for the research of various biochemical[1][2].
Lats-IN-1 is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. Lats-IN-1 promotes Yap-dependent proliferation in postmitotic mammalian tissues[1].
TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKAG595R, TRKAG667C and TRKAF589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1G595R and BaF3-CD74-NTRK1G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM[1].
Mal-amido-PEG8-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CNDAC hydrochloride is a metabolite of the orally active agent sapacitabine, and a nucleoside analog[1].
Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%); also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity.IC50 value:Target:in vitro: SLV308 acted as a potent but partial D(2) receptor agonist (pEC(50) = 8.0 and pA(2) = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D(3) receptors, SLV308 acted as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA(2) = 9.0). SLV308 acted as a full 5-HT(1) (A) receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT(1) (A) receptors but with low potency (pEC(50) = 6.3) [1].in vivo: Unified PD Rating Scale (UPDRS)-Motor score was improved in pardoprunox-treated patients (overall mean dose 23.8 mg/d; -7.3 points), as compared with placebo (-3.0 points; P = 0.0001), from baseline to end point. At end point, there were more responders (> or = 30% reduction in UPDRS-Motor score) in the pardoprunox group (50.7%) than in the placebo group (15.7%; P < 0.0001) [2]. Surprisingly in the SNc, pardoprunox (10 μg kg?1, i.v.) either partially or fully suppressed the firing activity in two separate populations of DA neurons. Finally, in the DRN, pardoprunox (5-40 μg kg-1, i.v.) completely suppressed the firing activity of 5-HT neurons. Moreover, the selective 5-HT(1A) receptor antagonist WAY-100,635 prevented and reversed the effects of pardoprunox [3].
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors[1].
Butaxamine (Butoxamin) hydrochloride is a specific β2-adrenergic receptor blocker. Butaxamine hydrochloride inhibits the decreases in urine volume in ethanol-anesthetized, water-diuretic rats[1].
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis[1].
Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and can be used as CXCR2 agonist. Ac-Pro-Gly-Pro-OH elicits bactericidal activity and inhibits lung inflammation, reducing immune cell apoptosis. Ac-Pro-Gly-Pro-OH enhances the production of type 1 cytokines (IFN-γ and IL-12) but inhibits the production of proinflammatory cytokines. Ac-Pro-Gly-Pro-OH has the potential for the research of sepsis[1][2].
3,5,6-Trichloro-2-pyridinol (TCP) is the main degradation product of the herbicide Triclopyr and the insecticides Chlorpyrifos and Chlorpyrifos-methyl[1].
(E)-3,4-Dimethoxycinnamyl alcohol is an antimutagenic. (E)-3,4-Dimethoxycinnamyl alcohol has antimutagenic activity against furylfuramide, Trp-P-1, and activated Trp-P-1[1].
Pirolate is a histamine H1 receptor.
cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. And it is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively[1][2].
HEPES sodium, a nonvolatile zwitterionic chemical buffering agent, is broadly applied in cell culture. HEPES sodium is effective at pH 6.8 to 8.2. HEPES sodium is also a potent inducer of lysosome biogenesis[1][2][3].
Bertilimumab (CAT 213; iCo-008) is a human monoclonal antibody targeting eotaxin-1 (CCL11). Bertilimumab has the potential for allergic disorders research[1].
Tetrahydropyranyldiethyleneglycol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].