Chemicals & Small Molecules

AZD2281, also known as Olaparib, is a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor and an anti-cancer drug being tested in patients with mutations in the genes BRCA1 or BRCA2.

Rolipram is a selective, cell permeable inhibitor of cAMP-specific phosphodiesterase 4 (PDE4). PDE4 enzymes inactivate cyclic AMP (cAMP) via hydrolysis to 5'-AMP. Rolipram has two enantiomeric forms, R(-) and S(+). This product is the racemic mixture of the two enantiomers.

Soruberoylanilide Hydroxamic Acid (SAHA), or Vorinostat, is a histone deacetylase inhibitor and causes growth arrest and death of some transformed cells both in vitro and in vivo, with little or no toxic effects on normal cells.

Geldanamycin is an antibiotic and a potent antitumor compound. It inhibits pp60src tyrosine kinase, and it also binds specifically to heat shock protein Hsp90 and its GP96 homologue. It is known to inhibit protein maturation.

Afatinib, also known as BIW-2992, is an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinases. Afatinib suppresses EGF-induced EGFR phosphorylation and cellular proliferation in various cell lines, including EGFR-overexpressing and HER2-expressing cell lines A431, NIH-3T3-HER2, NCI-N87 and BT-474.

Vismodegib (GDC-0449) is a potent hedgehog (Hh) signaling pathway inhibitor.

MS-275, also known as Entinostat, is an inhibitor of histone deacetylases (HDACs) and preferentially inhibits HDAC1 over HDAC3. It does not inhibit HDAC8 (IC50 > 100 µM). It induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo. Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs like adriamycin, inhibitors of PARPs, or inhibitors of Hsp90.

U0126 is a selective inhibitor of mitogen-activated protein kinase kinases, MEK-1 and MEK-2. It is a weak inhibitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Abl, Cdk2 and Cdk4.

Cyclopamine inhibits activation of the Hedgehog response pathway by binding to and inhibiting the proto-oncogene Smoothened (SMO). The effects of oncogenic mutations that either activate SMO or inactivate the tumor suppressor Patched (Ptch) can be reversed by cyclopamine treatment. Cyclopamine has also been shown to induce apoptosis in colorectal adenoma cell lines, carcinoma-derived cell lines, and skin basal cell carcinomas and is being investigated as an anti-cancer drug.