PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM[1].
ATP-Red 1 is a multisite-binding switchable fluorescent probe, and can selectively and rapidly responds to intracellular concentrations of ATP in living cells.
Decyl β-D-glucopyranoside is a glucofuran that interacts with bovine serum albumin (BSA). Decyl β-D-glucopyranoside has the ability to quench intrinsic fluorescence by forming a complex with BSA[1].
PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.
DNP-PEG3-DNP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DBCO-PEG4-triethoxysilane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Thrombin Receptor Activator for Peptide 5 (TRAP-5) is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).
Thalidomide-PEG5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
2-(1-Hydroxy-1-methylethyl)-4-methoxyfuro-[3,2-g]benzopyran-7-one is a compound isolated from sugarcane bagasse[1].
AZD7624 is an inhaled p38 inhibitor, with potent anti-inflammatory activity.
Polyporusterone C (Compound 3) is a natural product that can be isolated from Polyporus umbellatus. Polyporusterone C shows cytotoxic activities with IC50s of 37, 26 and 42 μg/mL against L-1210 cells at 3, 5 and 7 days, respectively[1].
MUT056399 is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively. IC50 value: 12 nM (for S. aureus), 58 nM (for E. coli) [1]Target: FabI enzymein vitro: MUT056399 is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli. MUT056399 is very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), linezolid-resistant, and multidrug-resistant strains, with MIC90s between 0.03 and 0.12 μg/ml. MUT056399 is also active against coagulase-negative staphylococci, with MIC90s between 0.12 and 4 μg/ml. MUT056399 is very active against the 118 S. aureus strains tested, including MSSA and MRSA isolates and linezolid-resistant and multidrug-resistant strains, with MIC90s between ≤0.03 and 0.12 μg/ml.In vivo: MUT056399, administered subcutaneously, protected mice from a lethal systemic infection induced by MSSA, MRSA, and vancomycin-intermediate S. aureus strains (50% effective doses ranging from 19.3 mg/kg/day to 49.6 mg/kg/day). In the nonneutropenic murine thigh infection model, the same treatment with MUT056399 reduced the bacterial multiplication of MSSA and MRSA in the thighs of immunocompetent mice.
SM-324405 is a TLR7 agonist, with pEC50 values of 7.3 and 6.6 for human TLR7 and Rat TLR7, respectively[1].
Sinensetin is a methylated flavone found in certain citrus fruits. pocess potent antiangiogenesis and anti-inflammatory, sinensetin enhances adipogenesis and lipolysis.In vitro: Sinensetin promots adipogenesis in 3T3-L1 preadipocytes growing in incomplete differentiation medium, sinensetin enhances adipogenesis and lipolysis by increasing cAMP levels. [1] Sinensetin shows anti-inflammatory activity by regulating the protein level of inhibitor κB-α (IκB-α). [2]In vivo: Sinensetin has the most potent antiangiogenesis activity and the lowest toxicity, inhibits angiogenesis by inducing cell cycle arrest in the G0/G1 phase in HUVEC culture and downregulating the mRNA expressions of angiogenesis genes flt1, kdrl, and hras in zebrafish. [3]
5’-O-DMTr-3’-deoxyuridine 2’-CED phosphoramidite 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].
Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
Tetrapeptide, an analogue of α-MSH, induces melanin synthesis. Tetrapeptide diminishes DNA damage by reducing the production of reactive oxidative species and enhancing repair of DNA photoproducts[1].
BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription[1].
2-Aminoacridone is a widely used fluorophore (λexc=428 nm, λem=525 nm).
Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research[1].
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth[1].
Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes[1][2][3][4].
2-((1H-1,2,4-Triazol-1-yl)methyl)-4-(4-chlorophenyl)-2-phenylbutanenitrile-d5 is the deuterium labeled 2-((1H-1,2,4-triazol-1-yl)methyl)-4-(4-chlorophenyl)-2-phenylbutanenitrile[1].
IGRP(206-214) is a biological active peptide. (This peptide corresponds to residues 206–214 of murine islet-specific glucose-6-phosphatase catalytic subunit–related protein (IGRP). This peptide is T cells specific for proinsulin and IGRP induces diabetes in non-obese diabetic (NOD) mice.)
(E)-7-Fluoro-4-hydrazono-4,5-dihydropyrrolo[1,2-a]quinoxaline is an intermediate, which can be used in the synthesis of SC144. SC144 is a potent agent with broad-spectrum cytotoxic activities in a number of tumor cells. SC144 shows excellent potency against a panel of human cancer cell lines[1].
ML324 is a potent JMJD2 demethylase inhibitor with demonstrated antiviral activity.IC50 value: 920 nM(JMJD2E) [1]Target: JMJD2 demethylase inhibitorML324 is a probe molecule that displays submicromolar inhibitory activity toward JMJD2E (in vitro) and possesses excellent in vitro ADME properties. In contrast to previously reported inhibitors of the JMJD proteins, ML324 displays excellent cell permeability providing an opportunity for more extensive cell-based studies of JMJD2 enzymes to be undertaken. In addition, ML324 demonstrates potent anti-viral activity against both herpes simplex virus (HSV) and human cytomegalovirus (hCMV) infection via inhibition viral IE gene expression. ML324 suppresses the formation of HSV plaques, even at high MOI, and blocks HSV-1 reactivation in a mouse ganglia explant model of latently infected mice.
Tubeimoside III, a triterpenoid saponin isolated from a Chinese folk medicine"Tubeimu", shows anti-inflammatory, anti-tumor, anti-tumorigenic activities, and acute toxicity in vivo[1].
Stachyose hydrate act as a prebiotic to enhance the growth and activity of beneficial bacteria. Stachyose hydrate exhibit a hypoglycemic effect, and improve inflammation through modulating gut microbiota[1].