L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively[1]. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6[2]. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases[1][2][3].
Dibekacin sulfate is an aminoglycoside antibiotic derived from Kanamycin B (HY-B1174), has a broad-spectrum antibacterial activities. Dibekacin sulfate closely resembles Tobramycin (HY-B0441) structurally and is against some strains of Ps. Aeruginosa resistant to gentamicin[1][2].
Perlolyrin (Tribulusterine) is an alkaloid that can be isolated from dried fruits of Tribulus terrestris[1].
3-O-Methylellagic acid is a nature product isolated from Myrciaria cauliflora, with anti-inflammatory activity. 3-O-Methylellagic acid shows an inhibitory effect on glucose transport assay. 3-O-Methylellagic acid has antibacterial activity, with a MIC of 32 μg/mL for Staph. Aureus ATCC 25923[1][2][3].
Praeroside II is an angular-type pyranocoumarm glycoside. Praeroside II can be isolated from the n-butanol-extracts of P. praeruptorum Dunn. Praeroside II can be used for pharmacological study[1].
Niraparib (MK-4827) is a highly potent PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively.
Antidesmone is a isoquinoline alkaloid that can be isolated from Antidesma membranaceum[1].
2',3',5'-Tri-O-(t-butyldimethylsilyl)-4'-C-hydroxymethyl uridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models[1].
A novel small molecule STAT3 inhibitor that inhibits STAT3 DNA binding activity with IC50 of 1.16 uM, binds to the STAT3 coiled-coil domain (CCD); also inhibits G-CSF-induced STAT3 phosphorylation in AML cell lines with IC50 of 0.8-1.9 uM,
Ac-IETD-AMC is a fluorogenic caspase-8/granzyme B substrate containing the acetyl (Ac) moiety. Ac-IETD-AMC is frequently used to measure caspase-8 activity[1].
Hinnuliquinone is a C2-symmetric dimeric non-peptide fungal metabolite inhibitor of HIV-1 protease. Hinnuliquinone is a bis-indolyl-2,5-dihydroxybenzoquinone pigment, that can be isolated from Nodulisphorium hinnuleum[1][2].
Hexidium iodide, a fluorescent nucleic binding acid stain (excitation/emission ~ 518/600 nm), permeants to mammalian cells and selectively stains almost all gram-positive bacteria. Hexidium iodide can bind to the DNA of all bacteria after permeabilization by EDTA[1][2].
Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM.
mGluR3 modulator-1 (compound 3) is a mGluR3 modulator, with an EC50 of 1-10 μM in HEK293T-mGluR-Gqi5 Calcium Mobilization Assay[1].
Limaprost-d3 (17α,20-dimethyl-δ2-PGE1-d3) is the deuterium labeled Limaprost. Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research[1][2].
UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.IC50 Value: 120 nM (Kd) [1]Target: L3MBTL3 In vitro: UNC1215 binds L3MBTL3 with a K(d) of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a unique 2:2 polyvalent mode of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization [1].
Epetraborole hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding "to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase". It is intended for the treatment of infections caused by Gram-negative bacteria. Epetraborole hydrochloride is a bacteriostatic compound that can against a wide range of anaerobic and Gram-negative bacteria, including multidrug-resistant pathogens, such as extended-spectrum-β-lactamase-, metallo-β-lactamase-, and carbapenemase-producing organism.
Quercetin 3-O-β-D-(6''-p-coumaroyl)glucopyranosyl(1→2)-α-L-rhamnopyranoside (Quercetin-3-O-[2-O-(6-O-p-hydroxyl-E-coumaroyl)-D-glucosyl]-(1→2)-L-rhamnoside) is one of the major antioxidants of Ginkgo biloba leaves[1].
Torachrysone (Nakahalene; Trachrysone), a naphthalene, can be isolated from Cassia tora L[1].
Thrombin inhibitor 1 is a potent thrombin inhibitor (Ki=0.66 nM, 2xaPTT=0.43 μM).
Direct Blue 1 (Chicago Sky Blue 6B) is a counterstain for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1, structurally related to glutamate, is a potent and competitive VGLUT inhibitor without affecting plasma membrane transporters. Direct Blue 1 is the first small molecule PrP ligand capable of inhibiting Aβ binding[1].
27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). Liarozole dihydrochloride prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders[1].
Androstenediol 17-acetate is a synthetic anabolic-androgenic steroid and an androgen ester.
CH 5450 (Z-Ile-Glu-Pro-Phe-Ome) is a human chymase inhibitor.
Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research[1][2][3].
Bafilomycin A1, a macrolide antibiotic isolated from the Streptomyces species, is a specific inhibitor of vacuolar-type H+ ATPase.
(R)-3-(4-Bromophenyl)-3-((tert-butoxycarbonyl)amino)propanoic acid is a phenylalanine derivative[1].
N-Acetyladenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].