(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML)[1][2].
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models[1][2].
Lurasidone Metabolite 14283 hydrochloride is a major active metabolite of Lurasidone. Lurasidone is a FDA approved drug for the treatment of schizophrenia.
FSBA? hydrochloride is a useful reagent for the affinity labeling of adenine nucleotide binding proteins and is mainly applied in the study of purified The labeling and subsequent detection of? these proteins can be blocked by including an excess of MgATP, which competes with FSBA for nucleotidebinding sites[1].
Fluticasone propionate is a high affinity, selective GR (glucocorticoid receptor) agonist which is derived from fluticasone used to treat asthma and allergic rhinitis.Target: Glucocorticoid ReceptorFluticasone propionate is a corticosteroid derived from fluticasone used to treat asthma and allergic rhinitis. It is also used to treat eosinophilic esophagitis. Fluticasone propionate is a synthetic trifluorinated glucocorticoid. It is highly lipophilic (logp octanol/water 3.69). In studies the topical drug has been associated with burning, stinging, skin irritation, blisters, dryness, skin infection, infected eczema, viral warts,impetigo, atopic dermatitis, pruritus, exacerbation of pruritus, exacerbation of eczema, erythema, and folliculitis.There are also numerous side effects associated with the oral version of this medication including headache, stuffy or runny nose, difficulty speaking, sore or irritated throat and painful white patches in the mouth or throat. Candidiasis of mouth and throat is reported as a "very common" side effect indicating that it occurs with a frequency greater than 1 in 10.Hoarseness is "common" indicating a frequency from 1 in 10 to 1 in 100. In both instances rinsing the mouth with water immediately after inhalation is recommended.
2’-Amino-2’-deoxy-5-methylcytidine is a purine nucleoside analogue. 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].
Xipamide is a sulfonamide-based diuretic. Xipamide is an antihypertensive agent able to selectively inhibit the anion exchanger (AE)[1].
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
5-Amino-2-((tert-butoxycarbonyl)amino)-5-oxopentanoic acid is a glutamine derivative[1].
Cyclo(Asp-Asp) is aCyclic dipeptide.
N2-iso-Butyroyl-7'-O-DMT-morpholinoguanine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[1]. 1-Octanol is a highly attractive biofuel with diesel-like properties[2].
Podophyllotoxin glucoside is a podophyllotoxin derivative, has anti-tumor effects[1].
[18F]-Labeled L-dopa precursor is a precursor for synthesis of 18F-labeled L-dopa extracted from patent WO2014095739A1, example 8[1].
Dihydrocurcumenone is a carabrane-type sesquiterpene. Dihydrocurcumenone can be isolated from Curcuma zedoaria, and the common form is 4-dihydrocurcumenone. Curcuma zedoaria sesquiterpene has vascular relaxation activity. 4-dihydrocurcumenone can inhibit the high concentration of K+ induced constriction of isolated rat aortic strips[1].
Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM)[1].
Idelalisib D5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor[1].
5'-O-TBDMS-N2-ibu-dG is a nucleoside derivative and can be used for lead compounds synthesis with anti-bovine viral diarrhea virus activity[1].
Baloramotide is a recombinant NY-ESO-1 protein containing 182 amino acids. Baloramotide increases the immune response against tumors[1].
Tranylcypromine hemisulfate is an irreversible, nonselective MAO inhibitor used in the treatment of depression.
4’-Azido-2’-deoxy-2’-fluoro-beta-D-arabinouridine is a uridine analogue. 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].
SYK/JAK-IN-1 is dual SYK/JAK inhibitor with IC50s of <5 nM for SYK and JAK2, respectively[1].
Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity[1][2][3].
Orexin receptor antagonist 2 (compound 30) is a potent orexin receptor antagonist with pKis of 7.69 and 9.78. Orexin receptor antagonist 2 has the potential for the research of insomnia[1].
N-benzoyl-L-aspartic acid, a major metabolite of benzyl glucosinolate, can be used for modification of peptides or proteins[1].
Azapropazone is a nonsteroidal anti-inflammatory drug (NSAID). Azapropazone can be used for the research of rheumatoid arthritis and other rheumatoid conditions[1].
Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis[1].
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes[1][2].
Methyl rosmarinate is a noncompetitive tyrosinase inhibitor which is isolated from Rabdosia serra, with an IC50 of 0.28 mM for mushroom tyrosinase, and also inhibits a-glucosidase[1].
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity[1].