Bioactive molecules

CAT # Product Name Description
CPD2806 BI-167107 BI-167107 is a β-Arrestin-Biased D2R Agonist. Targeting the D2R mediated activation of β-arrestin-2 might therefore be a valuable approach for the design of novel antiparkinsonian drugs.
CPD3237 CDDU-Me
CPD3611 SB-204990 SB-204990 is the prodrug of the potent ATP citrate-lyase inhibitor SB-201076. SB-204990, when administered orally to rats, was absorbed into the systemic circulation, pharmacologically relevant concentrations of SB-201076 were recovered in the liver. SB-204990 (25 mg/kg per day) also decreased plasma cholesterol levels (by up to 23%) and triglyceride levels (by up to 38%) in the dog, preferentially decreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels. SB-204990 is an important enzyme in controlling substrate supply for lipid synthesis de novo and a potential enzyme target for hypolipidaemic intervention.
CPD3619 CPD3619
CPD3236 CPD3236
CPD3235 CPD3235
CPD3234 BAY-545 BAY-545 is a potent and selective antagonist of the A2B adenosine receptor
CPD3232 NTN21277 NTN21277, also known as Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).
CPD3233 AZD-3409 AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma.
CPD3219 EW-7197 Hydrochloride EW-7197 Hydrochloride is a highly potent, selective, and orally bioavailable inhibitor of TGF-β type 1 receptor kinase.
CPD3218 BMS-955176 GSK3532795, also known as BMS-955176, is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb clinical trials. GSK3532795 combines broad coverage of polymorphic viruses (EC50 <15 nM toward a panel of common polymorphisms representative of 96.5% HIV-1 subtype B virus) with a favorable pharmacokinetic profile in preclinical species.
CPD3618 TAS-120 TAS-120 is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor TAS-120 selectively and irreversibly binds to and inhibits FGFR, which may result in the inhibition of both the FGFR-mediated signal transduction pathway and tumor cell proliferation, and increased cell death in FGFR-overexpressing tumor cells. FGFR is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival and its expression is upregulated in many tumor cell types.
CPD1609 SB-423562 SB-423562 is a calcium-sensing receptor antagonist potentially for the treatment of autosomal dominant hypocalcemia
CPD3616 CPD3616
CPD3508 GSK547 GSK547 is a highly selective and potent inhibitor of RIP1 kinase that targets RIP1 in vivo
CPD2801 OSI-027 OSI-027 is an orally bioavailable mammalian target of rapamycin (mTOR) kinase inhibitor with potential antineoplastic activity. mTOR kinase inhibitor OSI-027 binds to and inhibits both the raptor-mTOR (TOR complex 1 or TORC1) and the rictor-mTOR (TOR complex 2 or TORC2) complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR is a serine/threonine kinase that is upregulated in some tumors and plays an important role downstream in the PI3K/Akt/mTOR signaling pathway. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
CPD3504 BAY-218
CPD2807 BAY-293 BAY-293 is a potent SOS1 inhibitor that blocks RAS activation via disruption of the RAS-SOS1 interaction. BAY-293) selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM and is a valuable chemical probe for future investigations.
CPD2809 CPD2809 AMG-510 is a potent KRAS G12C covalent inhibitor. AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant. This may inhibit growth in KRAS p.G12C-expressing tumor cells
CPD1815 BI-3812 BI-3812 is a potent inhibitor of the interaction of the BTB/POZ domain of BCL6 with several co-repressors. It acts by inhibiting the BCL6::Co-repressor complex formation.
CPD2206 Selpercatinib Selpercatinib is a tyrosine kinase inhibitor with antineoplastic properties
CPD2500 Olutasidenib Olutasidenib is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 for the treatment of acute myeloid leukemia
CPD2047 VK2809
CPD2053 MB-07811 MB-07811, also known as MB-07344, is a thyroid hormone receptor beta (TRB) agonist potentially for the treatment of hyperlipidemia. The prodrug [MB07811] of a novel phosphonate-containing thyroid hormone receptor agonist [MB07344] is the first application of the HepDirect liver-targeting approach to a non-nucleotide agent.


Contact Us

Inquiry

Latest News

  • Top 7 Trends In Pharmaceutical Research In 2018

    Top 7 Trends In Pharmaceutical Research I...

      Being under ever-increasing pressure to compete in a challenging economic and technological environment, pharmaceutical and biotech companies must continually innovate in their R&D programmes to stay ahead ...

  • ARS-1620: A promising new inhibitor for KRAS-mutant cancers

    ARS-1620: A promising new inhibitor for K...

    According to a study published in Cell, researchers have developed a specific inhibitor for KRASG12C called ARS-1602 that induced tumor regression in mice. “This study provides in vivo evidence that mutant KRAS can be...

  • AstraZeneca receives regulatory boost for oncology drugs

    AstraZeneca receives regulatory boost for...

    AstraZeneca received a double boost for its oncology portfolio on Tuesday, after US and European regulators accepted regulatory submissions for its drugs, the first step towards winning approval for these medicines. ...

WhatsApp Online Chat !