AR-C66096 (FPL 66096) tetrasodium is a selective platelet P2YT receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism[1].
Nampt-IN-9 (Compound 8) is a potent NAMPT inhibitor with anticancer activities. Nampt-IN-9 can be used for pancreatic ductal adenocarcinoma research[1].
mTOR inhibitor-13 (compound 9g), an aryl ureido compound, is a potent and selective mTOR inhibitor with an IC50 of 0.29 nM. mTOR inhibitor-13 also inhibits PI3K-α with an IC50 of 119 nM[1].
L-threo-Sphingosine is a potent MAPK inhibitor. L-threo-Sphingosine induces apoptosis and clear DNA fragmentation. L-threo-Sphingosine shows anticancer effect[1].
PYBG-TMR is a dye and has a role as a fluorochrome. PYBG-TMR specifically and efficiently labels the target genetically encoded SNAP-tags in live cells[1].
RB-6145 is an orally active pro-drug of the hypoxic cell radiosensitizer RSU 1069. RB-6145 acts a hypoxic cell radiosensitizer and cytotoxin but reduces systemic toxicity in mice[1].
GDC-4379 is a JAK1 inhibitor that can be used for the research of asthma[1].
Hydroxymethylenetanshiquinone is a abietane diterpene that can inhibits tumor cell proliferation[1].
PCSK9-IN-20 (Compound 3i) is a PCSK9 inhibitor with an IC50 of 3.96 µM. PCSK9-IN-20 decreases PCSK9 and increases LDLR protein expression in vitro[1].
OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation .target: Wdr5IC 50: 5 uMIn vitro: OICR-9429 inhibit proliferation and induce differentiation in p30-expressing human AML cells. OICR-9429 cause a significant decrease in viability in the majority of patient cells with mutations in the N-terminal part of the CEBPA gene. OICR-9429 displays exquisite cellular selectivity and specificity in disrupting critical protein-protein interactions between WDR5. [1] reduce the viability of primary human AML cells with N-terminal C/EBPα mutations by about 50% (mean value, n = 8) at 5 μM[2]In vivo:The reference for OICR-9429 to mice (female NOD-SCID) is 3 mg/kg.
SAFit1 is a FK506 binding protein 51 (FKBP51)-specific inhibitor with a Ki of 4±0.3 nM[1][2].
Bdp tr nhs ester is a chemiluminescent coupling compound with a long excited state lifetime for immunoassays and is suitable for microscopy and fluorescence polarization analysis applications. NHS ester can react specifically and efficiently with the side chains of primary amines such as lysine residues or amino silane coated surfaces under neutral or weakly basic conditions to form covalent bonds[1].
Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo[1].
Diphtheria toxin CRM197, a nontoxic variant of diphtheria toxin, has a single mutation (Glycine to Glutamate substitution at position 52) that eliminates its toxicity. CRM197 is widely used as a carrier protein in conjugate vaccines[1].
Sodium benzoate can be used as an excipient, such as antimicrobial agent, preservative, lubricant. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1].
AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release[1][2].
BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure[1].
Tadnersen (BIIB078), an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion[1].
Adenosine receptor antagonist 4 (compound 2) is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor[1].
Triacsin C (WS 1228A), a natural intracellular long-chain acyl-CoA synthetases (ACSL) inhibitor, is from Streptomyces aureofaciens. Triacsin C inhibits TAG accumulation into lipid droplets (LD) by suppressing ACSL activity[1]. Triacsin C is found to be highly effective against rotavirus replication[2].
AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.IC50 Value: Target: GABA receptorin vitro: AWD 131-138 dose-dependently stimulated GABA currents(Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM [1]. in vivo: AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels [2]. Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model [3].
2’-O-(2-Methoxyethyl) inosine 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].
6-Methylmercaptopurine riboside 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].
Sulfo-Cy3-Tetrazine is a click chemistry reagent containing an tetrazine group. Sulfo-Cy3-Tetrazine is water soluble cyanine fluorescence dye, which is an inverse electron demand [4+2] cycloaddition that takes place between tetrazine and trans-cyclooctene or other strained olefin.
Gelidoside is a acylsecoiridoid glucoside isolated from the aerial parts of Gentiana gelida[1].
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively[1].
TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B).
A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell.
[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM[1].
RDN2150 (Compound 25) is a ZAP-70 inhibitor (IC50: 14.6 nM). RDN2150 covalently binds to the C346 residue of ZAP-70. RDN2150 inhibits the expression of CD25 and CD69, and inhibits CD4+ T cell activation. RDN2150 can be used for research of psoriasis[1].