D-Erythrose-d2 is the deuterium labeled D-Erythrose[1].
KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively[1].
Purpurin is a natural anthraquinone compound from Rubia tinctorum L.. Purpurin has antidepressant-like effects[1].
Boc-Arg(di-Z)-OH can be used for the synthesis of amino acid. Boc-Arg(di-Z)-OH can be used for the research of inhibitors for processing proteinases. Boc-Arg(di-Z)-OH is coupled via the mixed anhydride (MA) with HGlu(OBzl)-Lys(Z)-Arg(Z,Z)-CH2Cl[1].
CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity[1].
IGF1Rtide can be used as a RET kinase substrate for RET kinase assays[1].
H-Pro-Glu-OH is a protein secreted by pathogenic mycobacteria through the Type VII secretion system. H-Pro-Glu-OH targets LipY lipases to the cell Surface via the ESX-5 Pathway[1].
AChE-IN-27 (compound 8c) is an AChE inhibitor (IC50=0.19 µM). AChE-IN-27 can be used in studies of neurological diseases such as alzheimer's disease, dementia, ataxia and myasthenia gravis[1].
Rostafuroxin(PST 2238) is a antihypertensive compound; Na,K-ATPase antognist;displaced [3H]ouabain from the dogkidney Na+,K+-ATPase with IC50 of 1.5 nM.IC50 value: 1.5 nM [1]Target: Na+,K+-ATPase modulator; ouabain antagonistin vitro: PST 2238 displaced [3H]ouabain from the dog kidney Na+,K+-ATPase receptor (IC50 ) 1.5X 10-6M), was devoid of cardiac inotropic activity in isolated guinea pig atria, and showed no affinity up to 10-4 M with general (R1, R2, a1, a2, A1, A2, M1, M2, H1, H2, 5-HT1, 5-HT2, Ca2+ channels, TXA2/PGH2, PAF, GABAA, GABAB, DA-NE-5-HT uptake, glutammate,glycine, benzodiazepine) and hormonal (estrogenic, progestinic, androgenic, mineralcorticoid) receptors [1]. At molecular level, in the kidney, Rostafuroxin antagonizes EO triggering of the Src-epidermal growth factor receptor (EGFr)-dependent signaling pathway leading to renal Na+-K+ pump, and ERK tyrosine phosphorylation and activation [3].in vivo: PST 2238, given orally at very low doses (1 and 10 microg/kg for 5-6 weeks), reduced the development of hypertension in MHS rats and normalized the increased renal Na,K-ATPase activity and mRNA levels, whereas it did not affect either blood pressure or Na,K-ATPase in Milan-normotensive (MNS) rats [2].
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia)[1].
2α-Methyl androsterone is an anabolic androgenic steroid metabolite of mesterolone and drostanolone[1].
UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity[1].
Senazodan is a Ca2+ sensitiser, and also shows inhibition effect on PDE III.
T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively.
Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin[1][2][3].
Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC)[2].
Acantrifoside E (Compound 8) is a nature compound. Acantrifoside E can be isolated from the 90% ethanol extract of Salacia cochinchinensis. Acantrifoside E has none α-glucosidase inhibitory activity[1].
Ticlopidine (PCR 5332), an antithrombotic prodrug, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 µM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 µM and 149 µM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
6-Formyllimetin is a natural product isolated from the root bark of T. asiatica LAM[1].
H-Ser(tBu)-OtBu.HCl is a serine derivative[1].
SARS-CoV-2-IN-18 (Compound 26) is a potent SARS-CoV-2 3C-like protease inhibitor with an IC50 of 45 nM[1].
PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity[1][2].
PROTAC BRD4 Degrader-1 is an efficacious BRD4 degrader with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression[1].
M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors[1].
AAV2 Epitope is a biological active peptide. (This peptide is the capsid derived immunodominant adeno-associated virus 2 (AAV2), CD8 T cell epitope. Liver toxicity observed in a clinical trial of AAV2 delivered systemically to patients with hemophilia was ascribed to killing of vector-transduced hepatocytes by capsid-specific T-cells.)
N1-Allylpseudouridine 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].
ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.IC50 value:Target: TRPC4/C5 inhibitorML204 inhibited TRPC4β-mediated intracellular Ca(2+) rise with an IC(50) value of 0.96 μm and exhibited 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation. In whole-cell patch clamp recordings, ML204 blocked TRPC4β currents activated through either μ-opioid receptor stimulation or intracellular dialysis of guanosine 5'-3-O-(thio)triphosphate (GTPγS), suggesting a direct interaction of ML204 with TRPC4 channels rather than any interference with the signal transduction pathways. Selectivity studies showed no appreciable block by 10-20 μm ML204 of TRPV1, TRPV3, TRPA1, and TRPM8, as well as KCNQ2 and native voltage-gated sodium, potassium, and calcium channels in mouse dorsal root ganglion neurons. In isolated guinea pig ileal myocytes, ML204 blocked muscarinic cation currents activated by bath application of carbachol or intracellular infusion of GTPγS, demonstrating its effectiveness on native TRPC4 currents [1]. ML204 blocked TRPC4 channels in an electrophysiological assay with an IC value of 2.6 μM and was also active in fluorescent and electrophysiological assays in which TRPC4 channels were activated by different mechanisms, indicating direct block of TRPC4 channels. Selectivity for block of TRPC4 channels was examined in fluorescent and electrophysiological experiments against closely related TRPC channels and more distantly related TRPV, TRPA and TRPM channels, and against non-TRP ion channels. ML204 afforded good selectivity (19-fold) against TRPC6 channels and more modest selectivity against TRPC3 and TRPC5 (9-fold) channels [2].
α-Galactosidase (EC 3.2.1.22), that is, α-galactosidase, is a glycoside hydrolase that widely exists in animals, plants and microorganisms, and is often used in biochemical research. α-Galactosidase catalyzes the hydrolysis of α-1,6-linked terminal galactose residues, including galactooligosaccharides, galactomannans, and galactolipids. Catalyzes many catabolic processes including cleavage of glycoproteins, glycolipids and polysaccharides[1].
AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB[1].
Itanapraced (CHF5074) is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.