Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis[1][2][3].
C29 is a Toll-like receptor 2 (TLR2) inhibitor.
(Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide[1][2].
Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta.IC50 value:Target: ERbeta agonistin vitro: Treatment with ERβ selective estrogen agonists liquiritigenin and ERB-041 reduced the ability to invade a reconstituted basement membrane and to migrate in response to the cellular stimulus [1]. Pretreatment the PMs with ERB-041 resulted in a significant inhibition of LPS-induced iNOS expression and NF-kappaB activation by preventing its nuclear translocation [3].in vivo: Tumor numbers and volume were reduced by 60% and 84%, respectively, in the Erb-041-treated group as compared with UVB (alone) control. This inhibition in tumorigenesis was accompanied by the decrease in proliferating cell nuclear antigen (PCNA), cyclin D1, VEGF, and CD31, and an increase in apoptosis [2].
GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD)[1].
Cucurbitacin IIa is a triterpene isolated from Hemsleya amalils Diels, induces apoptosis of cancer cells, reduces expression of survivin, reduces phospho-Histone H3 and increases cleaved PARP in cancer cells[1].
BN82002 is a synthetic inhibitor of CDC25 phophatases, with IC50s of 2.4-6.3 μM for recombinant CDC25 phosphatases.
3’-O-(2-Methoxyethyl)-2-thiouridine 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].
PNU-282987 (free base) (Compound C7) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM[1].
Zedoarofuran is a natural product that can be isolated from Zedoariae Rhizoma[1].
Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis[1].
Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity[1][2].
AZD-5991 S-enantiomer is the less active enantiomer of AZD-5991. AZD-5991 S-enantiomer is a Mcl-1 inhibitor with an IC50 of 6.3 μM in FRET assay and a Kd of 0.98 μM in surface plasmon resonance (SPR) assay.
L-Glutamic acid monosodium salt (Monosodium glutamate) is an activator of mGlu1 receptor.
((3-Chloro-4-fluorophenyl)sulfonyl)proline is a proline derivative[1].
Litoxetine (SL 81.0385) is a selective 5-HT uptake inhibitor. Litoxetine is a 5-HT3 receptor antagonist with a Ki of 85 nM for cerebral 5-HT3 receptors. Litoxetine is an antidepressant and has antiemetic properties[1].
INCB-057643 is a novel, orally bioavailable BET inhibitor.
Cudraxanthone L is a natural flavanone compound[1].
β,β-Trehalose-d14 is the deuterium labeled β,β-Trehalose[1].
(S)-2-((tert-Butoxycarbonyl)amino)pent-4-ynoic acid is a Glycine (HY-Y0966) derivative[1].
Feglymycin is a HIV replication inhibitor. Feglymycin is also an antibiotic peptide that has antibacterial activity (MIC: 32-64 μg/mL for Staphylococcus aureus)[1].
Hydrastinine is a major alkaloid constituent in goldenseal (Hydrastis canadensis). Hydrastinine can be used as a haemostatic agent[1].
HIV Protease Substrate I is a chromogenic substrate of HIV-1 protease. HIV Protease Substrate I has the cleavage site of HIV protease[1].
eIF4A3-IN-17 (compound 61) is a silvestrol (HY-13251) analogue. eIF4A3-IN-17 interferes the assembling of eIF4F translation complex with EC50s of 0.9, 15 and 1.8 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-17 can be used for the research of human cancer pathogenesis[1].
Yadanziolide A, isolated from the cultivated dry seeds of Brucea javanica, has strong antiviral activities with IC50 of 5.5 μM against tobacco mosaic virus. Yadanziolide A shows significant antitumor effects[1][2].
Amaronol B is an auronol that can be isolated from the bark of Pseudolarix amabilis[1].
AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.IC50 value: Target: Lck inhibitorIn several other in vitro assays, AMG-47a displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 μM, AMG-47a effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
Anifrolumab is a type I interferon (IFN) receptor antagonist, a human monoclonal antibody. Anifrolumab blocks the activity of type I interferon. Anifrolumab can be used in systemic lupus erythematosus (SLE) research[1][2].
Galidesivir hydrochloride (BCX 4430 hydrochloride) is a viral RNA-dependent RNA polymerase (RdRp) inhibitor; demonstrated broad-spectrum activity in multiple viruses and a favorable preliminary preclinical safety profile.
H-Asp(Obzl)-OtBu.HCl is an aspartic acid derivative[1].