T6271

Tipifarnib (IND 58359) is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.

OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist with antidepressant-like activity, showing high affinity for the sigma receptor σ1/2 (IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM).

OPC-14523 dihydrochloride is the dihydrochloride form of the free base OPC-14523. OPC-14523 dihydrochloride is an orally active dual agonist of sigma receptors and 5-HT₁A receptors that also inhibits the 5-HT transporter, with IC₅₀ values of 47/56 nM for sigma receptors σ1/2, 5-HT₁A receptor IC₅₀ = 2.3 nM, and 5-HT transporter IC₅₀ = 80 nM. OPC-14523 dihydrochloride exhibits antidepressant-like activity. OPC-14523 dihydrochloride can be used in neuroscience research, including studies on antidepressants and neuroprotection.

Antitrypanosomal agent 6 (compound 18a) is a potent antitrypanosomal agent demonstrating good ADME properties, with an IC50 of 0.47 μM against Trypanosoma brucei (T. brucei), making it more than twice as active as Nifurtimox; it also exhibits a strong interaction with and selective binding to AT-rich DNA.

SOS1-IN-10 is a potent inhibitor of SOS1, targeting KRAS G12C-SOS1 with an IC50 of 13 nM.

Y08175 is a potent inhibitor of CBP Bromodomain. y08175 has an IC50 of 37 and 178.15 nM against CBP in the AlphaScreen and HTRF assays, respectively. y08175 can be used to study prostate cancer.

IRAK4-IN-20 is a potent and orally active IRAK4 inhibitor (IC50:3.55 nM). IRAK4-IN-20, which has anti-inflammatory, antitumor and anticancer effects, is often used to treat acute respiratory distress syndrome (ARDS).

BPTF-IN-1 (compound AU1) is a selective BPTF bromodomain inhibitor (Kd: 2.8 μM) that is more selective for BPTF than for the BRD4 bromodomain.BPTF-IN-1 has an antimalarial effect.

BTK-IN-10 is a potent inhibitor of BTK, effective against both wild-type BTK (IC50<5 nM) and mutant BTK (C481S) (IC50<5 nM).

A2AAR/HDAC-IN-2 is a potent dual A2AAR/HDAC inhibitor with good affinity for A2AAR (Ki: 10.3 nM) and effective HDAC1 inhibition (IC50: 18.5 nM). A2AAR/HDAC-IN-2 is applicable in anti-tumour studies.

RSK2-IN-3 (Compound 26) is a covalent, reversible inhibitor of the RPS6KA3 (RSK2) kinase.

AChE/BACE1/GSK3β-IN-1 is an orally active, blood-brain barrier-permeable, moderately bioavailable triple inhibitor of AChE, BACE1, and GSK3β, utilized for Alzheimer's disease (AD) research.