Aurora Kinase Inhibitor

Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC₅₀=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.

Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC₅₀ of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC₅₀ of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.

Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC₅₀s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.

Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with K_is of 0.6, 18, 4.6 nM, respectively.

MKI-3 is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC₅₀ of 5.72 nM and a K_d of 1.89 nM. MKI-3 disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 is applicable to research related to triple-negative breast cancer.

Ceftriaxone sodium salt (Ro 13-9904) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium salt is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 μM. Ceftriaxone sodium salt is an inhibitor of Aurora B. Ceftriaxone sodium salt has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium salt can be used in the study of bacterial infections and meningitis.

Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.

Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis.

JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC₅₀s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.

ZM-447439 is an aurora kinase inhibitor with IC₅₀s of 110 and 130 nM for aurora A and B, respectively.

Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC₅₀ of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.

Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC₅₀ of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC₅₀ of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.

KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABL^T315I and Aurora kinase with IC₅₀s of 6.6, 14, 4 and 48 nM, respectively.

AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC₅₀s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.

LY3295668 (AK-01) is a highly specific and orally active inhibitor of Aurora-A kinase with a K_i values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer.

MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC₅₀ value of 0.064 nM.

GRK6-IN-1 (Compound 18) is the inhibitor for G protein-coupled receptorkinase 6 (GRK6) with an IC₅₀ of 3.8-8 nM. GRK6-IN-1 also inhibits GRK7, GRK5, GRK4 and GRK1 with IC₅₀s of 6.4, 12, 22 and 52 nM, respectively. GRK6-IN-1 has the potential for the research of multiple myeloma.

PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a K_i of 0.49 nM, it is also a Chk2 inhibitor, with a K_i of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC₅₀=8 (K_i), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.