Triamcinolone hexacetonide is a commonly used long-acting steroids in treatment of subacute and chronic inflammatory joint diseases.
D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
Delcorine is a C19-diterpenoid alkaloid, which can be isolated from the whole herb of Delphinium anthriscifolium var. savatieri[1].
Lys-Phe-Glu-Arg-Gln can enhance the degradation of cytosolic proteins in human diploid fibroblasts deprived of serum[1].
LL-Z1640-4 is a potent p38/JNK signaling inhibitor. LL-Z1640-4 significantly diminishes p38 and JNK activation in HCC cells transfected with MLK4 siRNA. LL-Z1640-4 markedly attenuates ROS production induced by MLK4 knockdown. LL-Z1640-4 significantly reduces the apoptotic cells in HCC cells transfected with siMLK4[1][2].
Integrin signaling inhibitor, mP13 is an inhibitor of integrin signaling. Integrin signaling inhibitor, mP13 inhibits inside-out and outside-in signaling, including fibrinogen binding, platelet adhesion, and clot retraction[1].
Clenoliximab (IDEC-151) is a macaque-human chimeric monoclonal antibody (immunoglobulin G4) specific for the CD4 molecule on the surface of T lymphocytes. Clenoliximab can be used for the research of rheumatoid arthritis[1].
NH-bis-PEG2 is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Nebacumab (HA-1A) is a monoclonal antibody that binds to lipid A portion of endotoxin. Nebacumab can be used of research of sepsis[1][2].
CP-28888 is an interferon inducer, more potent in mice, but is less active in man and devoid of antirhinovirus effects.
Kadsurin A analogue-1 (Compound 8) is a lignan can be extracted from Piper argyrophylum[1].
DiSBAC10 is a voltage-sensitive fluorescent probe used to study cell membrane electrical activity in FRET assays. In a resting polarized cell, DiSBAC10 resides on the outer leaflet of the membrane where it accepts photons from excited fluorescein-labeled proteins and re-emits the photons at a higher wavelength. Depolarization of the cell causes rapid translocation of DiSBAC10 to the inner leaflet of the membrane, thereby increasing the distance between fluorophores and reducing the FRET signal.
Sirt1/2-IN-1 (Compound 7) is a SIRT1 and SIRT2 inhibitor with IC50 values of 1.81, 2.10 and 20.5 µg/mL against SIRT1, SIRT2 and SIRT3, respectively. Sirt1/2-IN-1 displays activity in hyperacetylation of α-tubulin protein with an IC50 of 32.05 µg/mL. Sirt1/2-IN-1 shows prominent anticancer activity[1].
Lobeglitazone is a new type of thiazolidinedione. Lobeglitazone can be used to prevent type 2 diabetes mellitus (T2DM)[1].
Tridodecyl methyl ammonium chloride is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS). compound (6R,12aS) is a potent PDE5 inhibitor with an IC50 of 0.090 μM, while ent-Tadalafil is inactive at concentrations up to 10 µM[1].
Glucagon receptor antagonists-4 is a highly potent glucagon receptor antagonist. It displays low in vivo clearance and excellent oral bioavailability in both rats and dogs.
Ixabepilone is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors[1].
UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.IC50 value: 1 uM(81 ± 10 % inhibition) [1]Target: KMO inhibitorin vitro: BFF 122 inhibited KAT activity almost completely at both 1 and 0.1 mM. The effect was still remarkable at 0.01 mM (70 ± 1 % inhibition). At the same three concentrations, BFF 122 did not affect KMO activity significantly. In contrast, UPF 648 totally blocked KMO at 0.1 and 0.01 mM and was still highly active at 0.001 mM (81 ± 10 % inhibition), but the compound was essentially ineffective at blocking KAT activity [1]. UPF 648 binds close to the FAD cofactor and perturbs the local active-site structure, preventing productive binding of the substrate l-kynurenine. Functional assays and targeted mutagenesis reveal that the active-site architecture and UPF 648 binding are essentially identical in human KMO, validating the yeast KMO-UPF 648 structure as a template for structure-based drug design [3].in vivo: Applying an identical experimental design, separate rats were used to study the effect of KMO inhibition on the de novo synthesis of KP metabolites in the lesioned striatum. These animals were bilaterally injected with 0.1 mM UPF 648 and 3H-kynurenine in PBS. 0.1 mM UPF 648 significantly reduced the neosynthesis of 3-HK and QUIN in the lesioned striatum (by 77 % and 66%, respectively) and moderately (27%) but significantly increased the de novo formation of KYNA [1]. Administered to pregnant rats or mice on the last day of gestation, UPF 648 (50 mg/kg, i.p.) produced qualitatively similar changes (i.e., large increases in kynurenine and KYNA and reductions in 3-HK and QUIN) in the brain and liver of the offspring. Rat pups delivered by UPF 648-treated mothers and immediately exposed to neonatal asphyxia showed further enhanced brain KYNA levels [2]. UPF 648, has an IC50 of 20 nM and provides protection against intrastriatal QUIN injections in kynurenine aminotransferase (KAT II) deficient mice. UPF 648 treatment also shifts KP metabolism towards enhanced neuroprotective KYNA formation [3].
Momelotinib-d8 (CYT387-d8) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally acitve and ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively, shows much less activity against JAK3[1][2].
Anivamersen sodium is an RNA aptamer to reverse the anticoagulant effect of the parenteral factor IXa inhibitor pegnivacogin. REG1 is a novel anticoagulation system consisting of pegnivacogin, an RNA aptamer inhibitor of coagulation factor IXa, and anivamersen, a complementary sequence reversal oligonucleotide.
Scholaricine (compound 13 ) is an alkaloid isolated from the leaf and stem-bark extracts of Alstonia spatulata. Scholaricine reverse multidrug resistance in vincristine-resistant KB cells with an IC50 value of 13.35 μM[1].
Fosciclopirox suppresses growth of urothelial cancer by targeting the γ-secretase complex. Fosciclopirox selectively delivers the active metabolite, Ciclopirox (CPX), to the entire urinary tract[1][2]. Ciclopirox has anticancer activity in a number of solid and hematologic malignancies.
MrgprX2 antagonist-3 is an MrgprX2 antagonist extracted from patent WO2021092240A1, example E117. MrgprX2 antagonist-3 can be used for the research of inflammatory disorders of the skin[1].
GNE-6468 is a potent and selective RORγ(RORc) agonists with an EC50 value of 13 nM for HEK-293 cell.
β-Zearalanol-d4 is a deuterium labeled Beta-Zearalanol (HY-N6740）[1]. Beta-Zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells[2]. Beta-Zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid[3].
Denileukin diftitox (DAB 389IL-2) is a diphtheria toxin (DT)-related interleukin 2 (IL-2) fusion protein toxin that depletes cells expressing the high-affinity form of the IL-2 receptor (IL-2R), CD25. Denileukin diftitox binds to cells expressing IL-2R and inhibits protein synthesis through internalization of the diphtheria toxin fragment[1][2][3].
Deunirmatrelvir is a deuterium labeled compound.
Kulactone, a natural bioflavonoid and an inhibitor against jRdRp, possesses antifungal, antibacterial and antiplasmodial activities. Kulactone exhibit no crossing through Blood Brain Barrier (BBB)[1][2].