aurora-b

Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor (Ki <0.010 µM) with potential anticancer activity for cancer research.

KW-2450 Formate is an IGF-1R/IR tyrosine kinase inhibitor with antitumor effects that acts through inhibition of Aurora A and B kinases.KW-2450 Formate inhibits the growth of TNBC xenografts and induces tetraploid accumulation.

Ceftriaxone Sodium is a broad-spectrum β-lactam tertiary cephalosporin antibiotic with anti-inflammatory, antitumor, antibacterial, and antioxidant activities.Ceftriaxone Sodium is a covalent GSK3β and Aurora B inhibitor used in the study of sepsis and infective endocarditis.

SP-146 is a selective, potent and non-ATP-competitive Aurora B inhibitor(IC50 : 0.316 nM).

BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK PTK6), displaying an IC50 of 30 nM, and effectively suppresses p-SAM68 with an IC50 of 52 nM. This compound serves as a valuable tool for evaluating BRK inhibitors' efficacy in xenograft breast tumor models, enabling in vivo activity assessment.

LY3295668 (AK-01) is a selective inhibitor of Aurora A, with Ki values of 0.8 nM for Aurora A and 1038 nM for Aurora B.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor with a Ki of 0.59 nM.

TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM, demonstrating approximately 3,700-fold greater selectivity for Aurora B over Aurora A.

Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

Tozasertib (MK-0457) is a pan-Aurora kinase inhibitor (Kis: 0.6 18 4.6 nM for Aurora A Aurora B Aurora C). It shows selectivity against more than 190 different kinases.

TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).

Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A B C(IC50s=150-500 nM).

Hesperadin(IC50=250 nM) effectively inhibits Aurora B. It potently reduces the activity of AMPK, MAPKAP-K1, MKK1, Lck, CHK1 and PHK, but it could not inhibit MKK1 activity in vivo.

PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2 3.

SNS-314 Mesylate (SNS-314) is an effective and specific Aurora A/B/C inhibitor (IC50: 9/31/3 nM). It is less inhibition of Trk A/B, Fms, Flt4, c-Raf, Axl, and DDR2.

NU6140 is a selective inhibitor of CDK2-cyclin A (IC50, 0.41 μM). It shows 10- to 36-fold selectivity over other CDKs. NU6140 also effectively inhibits Aurora A and Aurora B (IC50s: 67 and 35 nM, respectively). It also enhances the apoptotic effect and has anti-cancer activity.

Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A Aurora B Aurora C (IC50s: 120 nM 7 nM 1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).

7-bromoindirubin-3'-oxime (7BIO) is a caspase independent nonapoptotic cell death inducer. 7BIO is an inhibitor of FLT3, DYRK1A, DYRK2, Aurora B and Aurora C kinases.

AAPK-25 is a potent and selective Aurora PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A -B -C with Kd values ranging from 23-289 nM.

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1 2 than HER4, less potent to MEK1 5, c-Met, Aurora B, Lck, CSK etc. Phase 1.

ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A B than MEK1, Src, Lck and has little effect against CDK1 2 4, Plk1, Chk1, etc.

SP-96 is a highly effective and selective inhibitor of Aurora B with an IC50 of 0.316 nM. SP-96 shows selective growth inhibition in NCI60 screening, including MDA-MD-468 (GI50=107 nM). SP-96 can be used in triple negative breast cancer studies.

(1E)-CFI-400437 dihydrochloride (CFI-400437 dihydrochloride) is a selective and potent polo-like kinase 4 (PLK4) inhibitor.

Aurora kinase inhibitor-2 (IUN-70219) is a cell-permeable anilinoquinazoline that inhibit the activity of Aurora A (IC50 = 0.39 M).

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. It also inhibits multiple kinases, including LCK (pIC50 5.4), LRRK2 (pIC50 5.4), GSK3β (pIC50 5.3), JAK2 (pIC50 5), VEGFR2 (pIC50 4.5), Aurora B (pIC50 <4.6), and Aurora A (pIC50 <4.3). Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.

JH295 is a highly potent and selective inhibitor of NIMA-related kinase 2 (Nek2), exhibiting irreversible inhibition activity with an IC 50 value of 770 nM. This compound effectively inhibits cellular Nek2 using the alkylation of Cys22. Importantly, JH295 does not exhibit any inhibitory effects toward Cdk1, Aurora B, or Plk1, which are kinases involved in mitotic processes. Furthermore, JH295 has no impact on bipolar spindle assembly or the spindle assembly checkpoint mechanism.

Aurora Kinases-IN-2 (compound 12Aj) is a potent inhibitor of Aurora kinases, with IC50 values of 90 nM for Aurora A and 152 nM for Aurora B, and is applicable in cancer research.

SCH-1473759 is an inhibitor of the aurora (IC50s: 4 and 13 nM for Aurora A and B, respectively).

SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A); 1 nM (Aurora B / incenp); 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expression. It induced significant modulation of Aurora A and Aurora B biomarkers (p-Aurora A and pHH3, respectively) and cell polyploidy, as expected from Aurora A/B inhibitors.

XMD-12, also known as DUN57447, Aurora inhibitor (compound 1) or Aurora-IN-1, is an Auroro inhibitor, which targets Aurora A/B/C. (5.6/18.4/24.6 nM).

CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc.

AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

11α-O-Tigloyl-12β-O-acetyltenacigenin B, an ester derivative isolated from Garcinia cambogia (MTC), modulates the antitumor effects of Aurora-A in lymphoma through its parent compound, Tenacigenin B.

Hesperadin hydrochloride is an ATP-competitive indolone inhibitor of Aurora A and B, with an IC50 value of 250 nM for Aurora B.

Centrinone (LCR-263) (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM).

BI-831266 is a potent and selective Aurora kinase B inhibitor.

JAK-IN-19 is a potent JAK inhibitor with pIC50 values of 7.2 for PBMC (IFNγ) and 7.7 for HLF (Eotaxin). The compound also exhibits pIC50 values of 7.0 for VEGFR2 and 5.8 for Aurora B.

BPR1K653 is a potent Aurora kinase inhibitor with potential anticancder activity. BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent activity against the growth of xenograft tumors of the human cervical carcinoma KB and KB-derived MDR1-positive KB-VIN10 cells in nude mice. Finally, BPR1K653 also exhibited favorable pharmacokinetic properties in rats., BPR1K653 is a promising anti-cancer compound that has potential for the management of various malignancies, particularly for patients with MDR1-related drug resistance after prolonged chemotherapeutic treatments.

Tripolin A is a specific non-ATP competitive inhibitor of Aurora A kinase(Aurora A and Aurora B with IC50 values of 1.5 μM and 7 μM, respectively)

CCT 137690 is a highly specific and oral-available aurora kinase inhibitor, for aurora A(IC50=15 nM ), B(IC50=25 nM) and C(IC50=19 nM).

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.

JB170, a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM), achieves its selectivity by linking Alisertib to the Cereblon-binding molecule Thalidomide. It demonstrates a strong preference for AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). The mechanism of JB170 involves S-phase arrest, specifically through AURORA-A depletion, and it is notably effective in inhibiting the non-catalytic functions of AURORA-A kinase [1].

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007)