Purinostat mesylate is a Selective HDAC Inhibitor With anti-Leukemia Effects
Purinostat mesylate is a selective inhibitor of HDAC. This compound inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate (1-10 μM) inhibits HDAC1, 2, 3, and 8. And the IC50s are 0.81, 1.4, 1.7, and 3.8 nM, respectively. It also inhibits HDAC6 and 10,...
PM-81I is a Potent STAT6 Inhibitor
The signal transducer and activator of transcription (STAT) belong to a group of latent cytoplasmic transcription factors that play a central role in transmitting signals from the cytoplasmic membrane to the nucleus. There are seven members of the STAT family: STAT1, STAT2, STAT3, STAT4, STAT5A, STAT5B, and STAT6. STAT...
Vamotinib (PF-114) is a Potent, Selective and Orally Active Tyrosine Kinase Inhibitor
BCR-ABL, a fusion gene, is a mutation that is formed by the combination of two genes, BCR and ABL. The BCR gene is normally on chromosome number 22. The ABL gene is normally on chromosome number 9. The BCR-ABL mutation happens when pieces of BCR and ABL genes break...
DD1 is a Proteasome Inhibitor Used for Acute Myeloid Leukemia (AML) Research
Acute myeloid leukemia (AML) is clinically and genetically heterogeneous hematopoietic cancer. Leukemia cells are unable to undergo growth arrest and terminal differentiation. The conventional chemotherapeutic approach for AML contains a combination of anthracycline with cytarabine. However, due to either refractory to front-line therapy or subsequent relapse, AML remains a...
Panobinostat is a Potent and Orally Active Non-selective HDAC Inhibitor
HDACs (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. This is important because acetylation and de-acetylation can regulate DNA expression. Acetylation is controlled by two antagonistic enzyme families:...
Epothilone B is a Microtubule Stabilizer
Microtubules are polymers of tubulin, which is one of several members of a small family of globular proteins. The tubulin superfamily includes five distinct families, the α-, β-, γ-, δ-, and ε-tubulins and a sixth family which is present only in kinetoplastid protozoa. The most common members α-tubulin and...
Nimbolide Induces Apoptosis through Inactivation of NF-κB
The transcription factor NF-κB is a nuclear factor that binds to the enhancer element of the immunoglobulin kappa light-chain of activated B cells. NF-κB exsists in nearly all cell types and regulates many target genes with a whole variety of functions. There are five members of the NF-κB family:...