Bioactive molecules

CAT # Product Name Description
CPD112243 CCR2 antagonist 3 CCR2 antagonist 3 is an antagonist of chemokine receptor 2 (CCR2).
CPD108542 Tirabrutinib; ONO-4059 Tirabrutinib (ONO-4059) is an orally effective, highly selective Bruton's Tyrosine Kinase (BTK) inhibitor.
CPD110808 RMC 0331; RM 023 RMC-0331 (RM-023) is a highly efficient, selective, and orally bioavailable SOS1 inhibitor.
CPD1599 CDDO-3-P-Im; CDDO-2P-Im CDDO-2P Im is a CDDO imidazole amine analogue with chemopreventive properties.
CPDB1593 Telaglenastat; CB-839 CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity.
CPD1598 CDDO Imidazolide; CDDO Im; RTA 403; TP 235 CDDO Im (RTA-403) is an activator of Nrf2 and PPAR.
CPD114656 (R)-Pirtobrutinib (R) Pirtobrutinib is a less active isomer of Pirtobrutinib. Pirtobrutinib is a highly selective and non covalent next-generation BTK inhibitor.
CPD2500 Olutasidenib; FT-2102 Olutasidenib is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 for the treatment of acute myeloid leukemia
CPD9951 Batefenterol;GSK 961081; TD-5959 Batefenterol is a muscarinic antagonist and β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4, 1.3, and 3.7 nM, for hM2, hM3, and hβ2-AR, respectively in a radioligand binding assay).
CPD3619 RTA dh404;CDDO-dhTFEA
CPD3236 methyl (4aS,6aR,6bR,8aR,12aR,12bR,14aR,14bS)-11...
CPD115153 NX-2127;zelebrudomidum; zelebrudomide NX-2127 is an orally effective BTK inhibitor.
CPDD0995 Bardoxolone methyl;RTA 402;NSC 713200;TP155;CDDOMe The synthetic oleanane triterpenoid CDDO (Item No. 81035) is a Nrf2 activator that inhibits proliferation and induces differentiation and apoptosis in various cancer cells.
CPD0854 Sotagliflozin;LX-4211 Sotagliflozin (LX-4211) is an SGLT1/2 inhibitor and an anti diabetes agent.
CPD1111 MAK683; EED inhibitor 1 MAK683 is an inhibitor of embryonic ectoderm development (EED)
CPD107768 Icotinib HCl;BPI2009 Icotinib Hydrochloride (BPI-2009) is an effective and selective EGFR inhibitor
CPD2809 AMG-510 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
CPD100230 JBJ-04-125-02 R-isomer
CPD102300 S-55746
CPD101235 diABZI STING agonist-1 trihydrochloride diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
CPD101234 diABZI STING agonist-1 (Tautomerism) diABZI STING agonist-1 Tautomerism (compound 3) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
CPD101233 diABZI STING agonist-1 diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.
CPD101232 STING agonist-4 STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function
CPD101231 STING agonist-3 STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer
CPD100904 Voruciclib Voruciclib, also known as P1446A-05, is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity. CDK4 inhibitor P1446A-05 specifically inhibits CDK4-mediated G1-S phase transition, arresting cell cycling and inhibiting cancer cell growth. The serine/threonine kinase CDK4 is found in a complex with D-type G1 cyclins and is the first kinase to become activated upon mitogenic stimulation, releasing cells from a quiescent stage into the G1/S growth cycling stage; CDK-cyclin complexes have been shown to phosphorylate the retinoblastoma (Rb) transcription factor in early G1, displacing histone deacetylase (HDAC) and blocking transcriptional repression.
CPD100905 Alvocidib Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity. Check for active clinical trials or closed clinical trials using this agent.
CPD100906 BS-181 BS-181 is a highly selective CDK inhibitor for CDK7 with an IC(50) of 21 nmol/L. Testing of other CDKs as well as another 69 kinases showed that BS-181 only inhibited CDK2 at concentrations lower than 1 micromol/L, with CDK2 being inhibited 35-fold less potently (IC(50) 880 nmol/L) than CDK7. In MCF-7 cells, BS-181 inhibited the phosphorylation of CDK7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines, and showed antitumor effects in vivo.
CPD100907 Riviciclib Riviciclib, also known as P276-00 , is a flavone and cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. P276-00 selectively binds to and inhibits Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation.
CPD100908 MC180295 MC180295 is a highly selective CDK9 inhibitor (IC50 = 5 nM). (MC180295 has broad anti-cancer activity in vitro and is effective in in vivo cancer models. Additionally, CDK9 inhibition sensitizes to the immune checkpoint inhibitor α-PD-1 in vivo, making it an excellent target for epigenetic therapy of cancer.
1073485-20-7 LDC000067 LDC000067 is a potent and selective CDK9 inhibitor. LDC000067 inhibited in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrated a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis. Analysis of de novo RNA synthesis suggested a wide ranging positive role of CDK9. At the molecular and cellular level, LDC000067 reproduced effects characteristic of CDK9 inhibition such as enhanced pausing of RNA polymerase II on genes and, most importantly, induction of apoptosis in cancer cells. LDC000067 inhibits P-TEFb-dependent in vitro transcription. Induces apoptosis in vitro and in vivo in combination with BI 894999.

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