Search Result
Results for "
Aurora A kinases
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-10971
-
Alisertib
Maximum Cited Publications
72 Publications Verification
MLN 8237
|
Aurora Kinase
Autophagy
Apoptosis
|
Cancer
|
|
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 .
|
-
-
- HY-10329
-
|
|
Aurora Kinase
CDK
Apoptosis
|
Cancer
|
|
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 .
|
-
-
- HY-10161
-
|
VX 680; MK-0457
|
Aurora Kinase
Autophagy
|
Cancer
|
|
Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.
|
-
-
- HY-14711
-
|
|
Aurora Kinase
Autophagy
|
Cancer
|
|
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.
|
-
-
- HY-10179
-
|
PHA-739358
|
Aurora Kinase
Autophagy
|
Cancer
|
|
Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
|
-
-
- HY-13253
-
AMG 900
4 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
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.
|
-
-
- HY-10180
-
|
|
Aurora Kinase
|
Cancer
|
|
MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
|
-
-
- HY-13252
-
-
-
- HY-10339
-
-
-
- HY-50514
-
|
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
|
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 .
|
-
-
- HY-130665
-
|
|
PROTACs
CDK
|
Cancer
|
|
TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM) .
|
-
-
- HY-10128
-
-
-
- HY-12003
-
|
|
Aurora Kinase
|
Cancer
|
|
SNS-314 mesylate is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
|
-
-
- HY-137377
-
TAS-119
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites .
|
-
-
- HY-124526
-
|
Ibcasertib; CS2164
|
PDGFR
c-Fms
Aurora Kinase
VEGFR
c-Kit
Mitosis
|
Cancer
|
|
Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects .
|
-
-
- HY-156863
-
-
-
- HY-112273
-
CD532
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer .
|
-
-
- HY-10804
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
|
-
-
- HY-13819
-
-
-
- HY-15749
-
-
-
- HY-123159
-
|
|
Aurora Kinase
|
Cancer
|
|
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .
|
-
-
- HY-145601
-
|
TT 00420
|
Aurora Kinase
FGFR
VEGFR
|
Cancer
|
|
Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment .
|
-
-
- HY-18161
-
|
|
FLT3
Aurora Kinase
|
Cancer
|
|
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
|
-
-
- HY-141512
-
JB170
3 Publications Verification
|
PROTACs
Aurora Kinase
|
Cancer
|
|
JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase .
|
-
-
- HY-142817
-
|
|
G Protein-coupled Receptor Kinase (GRK)
Aurora Kinase
|
Cancer
|
|
GRK6/Aurora A-IN-1 is a dual inhibitor of G protein-coupled receptor kinase 6 (GRK6)/Aurora A, with IC50 values of 120 nM and 11 nM, respectively. GRK6 is a key kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for research on multiple myeloma .
|
-
-
- HY-10178
-
|
|
Aurora Kinase
|
Cancer
|
|
PHA-680632 is an aurora kinase inhibitor with IC50s of 27, 135 and 120 nM for aurora A, B and C, respectively.
|
-
-
- HY-122236
-
|
|
Mitosis
Kinesin
Microtubule/Tubulin
Aurora Kinase
|
Cancer
|
|
UMK57 is a MCAK activator and kinetochore-microtubule destabilizer. UMK57 enhances MCAK-dependent microtubule depolymerization, increases kinetochore-microtubule turnover, reduces chromosome mis-segregation and lagging chromosomes, and inhibits cancer cell proliferation. UMK57 triggers adaptive resistance in Aurora B cancer cells via reversible Aurora B signaling pathway alterations. UMK57 can be used for the research of solid tumors .
|
-
-
- HY-151971
-
|
|
Aurora Kinase
Polo-like Kinase (PLK)
|
Cancer
|
|
Aurora kinase-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10 .
|
-
-
- HY-13072
-
|
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
-
- HY-125956
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurkin A is an allosteric inhibitor for the interaction between Aurora A Kinase (also known also Aurka) and TPX2, through targeting the TPX2 binding sites with Kd of 3.77 μM. Aurkin A can disrupt polyploidy induced by Alisertib (HY-10971) and increase apoptosis of tumor cells. Aurkin A can be used in research on mitosis and cancer .
|
-
-
- HY-112355
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively .
|
-
-
- HY-112373
-
|
|
Aurora Kinase
|
Others
|
|
Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket .
|
-
-
- HY-12049
-
|
|
Aurora Kinase
|
Cancer
|
|
CCT129202 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.
|
-
-
- HY-103266
-
|
|
Aurora Kinase
|
Cancer
|
|
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
|
-
-
- HY-112273A
-
|
|
Aurora Kinase
|
Cancer
|
|
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer .
|
-
-
- HY-W231513
-
|
|
MASTL
Ser/Thr Protease
Aurora Kinase
|
Cancer
|
|
MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis .
|
-
-
- HY-144991
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases.
|
-
-
- HY-175866
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora kinase-IN-8 is a orally active Aurora kinase inhibitor. Aurora kinase-IN-8 shows IC50 values of 2.8 and 28.1 nM against Aurora A kinase and Aurora B kinase. Aurora kinase-IN-8 can prevent spindle formation, cause G2/M phase arrest, and induce cell apoptosis. Aurora kinase-IN-8 can be used for the research of cancer, such as triple-negative breast cancer .
|
-
-
- HY-112809
-
|
|
Syk
Src
LRRK2
GSK-3
JAK
VEGFR
Aurora Kinase
|
Inflammation/Immunology
|
|
GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin .
|
-
-
- HY-175830
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
PROTAC AURKA degrader 1 (Compound A16 + X7) is a Aurora kinase A (AURKA) PROTAC degrader. PROTAC AURKA degrader 1 can be used for cancers research . Pink: AURKA ligand (HY-175827); Blue: CRBN ligase ligand (HY-W867704); Black: linker (HY-132208)
|
-
-
- HY-123610
-
|
|
Aurora Kinase
|
Cancer
|
|
BRD-7880 is a potent and highly specific inhibitor of Aurora Kinase B (AURKB) and Aurora Kinase C (AURKC), with IC50 values of 7 nM and 12 nM, respectively .
|
-
-
- HY-175526
-
|
|
Ligands for Target Protein for PROTAC
Aurora Kinase
|
Cancer
|
|
Aurora kinase ligand-1 (Compound I-4) is an Aurora kinase B (AURKB) PROTAC ligand. Aurora kinase ligand-1 can be conjugated with E3 ligase Ligand (HY-112078) and linker to synthesize AURKB PROTAC degrader MS44 (HY-175525). MS44 can be used for cancer research .
|
-
-
- HY-108344
-
|
|
Aurora Kinase
|
Cancer
|
|
SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
|
-
-
- HY-10971A
-
|
MLN 8237 sodium
|
Aurora Kinase
Autophagy
Apoptosis
|
Cancer
|
|
Alisertib (MLN 8237) sodium 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 sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
|
-
-
- HY-175827
-
-
-
- HY-149693
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-11 (compound 25) is an inhibitor of Aurora Kinase with an IC50 of 0.14 μM. Aurora kinase inhibitor-11 has anticancer activity .
|
-
-
- HY-158618
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia .
|
-
-
- HY-147703
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
|
-
-
- HY-111506
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively .
|
-
-
- HY-122370A
-
|
|
Aurora Kinase
|
Cancer
|
|
Tripolin B is an ATP-competitive Aurora kinase inhibitor with IC50 values of 2.5 µM and 6 µM for Aurora A and Aurora B kinases, respectively. Tripolin B does not inhibit Aurora kinase in cells .
|
-
- HY-149354
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora kinase-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora kinase-IN-4 can be used for research of triple negative breast cancer (TNBC) .
|
-
- HY-124330
-
|
(E)-Tripolin A
|
Aurora Kinase
|
Others
|
Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively .
|
-
- HY-N3737
-
-
- HY-10057
-
|
|
Aurora Kinase
|
Cancer
|
|
AT9283 hydrochloride is a multi-targeted kinase inhibitor with anti-tumor activity. AT9283 hydrochloride has been found to effectively inhibit Aurora A and Aurora B kinases, thereby affecting cell proliferation and survival. AT9283 hydrochloride can also inhibit several other kinases, including JAK2 and Abl (T315I) .
|
-
- HY-121895
-
|
|
Aurora Kinase
|
Cancer
|
|
BI 831266 is a potent and selective inhibitor of Aurora kinase B with antitumor activity .
|
-
- HY-164454
-
|
|
Aurora Kinase
STAT
JAK
Mitosis
|
Inflammation/Immunology
|
|
AJI-100 is a dual-target inhibitor of Aurora kinase A and JAK2 with IC50 values of 12.7 nM and 18.5 nM, respectively. AJI-100 directly blocks Aurora kinase A to inhibit T cell mitosis and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-100 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
|
-
- HY-N3634
-
|
|
EGFR
TAM Receptor
Tie
|
Cancer
|
|
Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .
|
-
- HY-129727
-
|
|
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Mitosis
|
Others
|
|
(E)-MS0019266 is a potent inhibitor of DNA damage repair. (E)-MS0019266 inhibits ribonucleotide reductase by generating reactive oxygen species. (E)-MS0019266 also reduces expression of genes related to cell cycle arrest and mitosis, including polo-like kinase 1, kinesin family member 20a, cyclin B1 and aurora kinase A. (E)-MS0019266 is promising for research of inhibitors of ribonucleotide reductase and polo-like kinase 1 .
|
-
- HY-169505
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-13 (Compound 2) is an inhibitor of Aurora kinase, with an IC50 value of 2.3 μM against Aurora kinase A .
|
-
- HY-144438
-
|
|
Aurora Kinase
LIM Kinase (LIMK)
|
Cancer
|
|
Aurora/LIM kinase-IN-1 (Compound F114) is a potent and dual inhibitor of aurora and lim kinase. Aurora kinases and lim kinases are involved in neoplastic cell division and cell motility, respectively. Aurora/LIM kinase-IN-1 inhibits GBM proliferation and invasion. Aurora/LIM kinase-IN-1 is a promising new scaffold for dual aurora/lim kinase inhibitors that may be used in future agent development efforts for GBM, and potentially other cancers .
|
-
- HY-150592
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase-IN-2 (compound 12Aj) is a potent Aurora kinase inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora kinase-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora kinase-IN-2 can be used for cancer research .
|
-
- HY-160447
-
|
|
Aurora Kinase
FAK
|
Cancer
|
|
FAK/Aurora kinase-IN-1 is a FAK and aurora kinase inhibitor with IC50 values of 6.61 nM and 0.91 nM, respectively. FAK/Aurora kinase-IN-1 shows anticancer effects (WO2018019252A1; compound 11) .
|
-
- HY-147993
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity .
|
-
- HY-149694
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-12 (Compound 1a ) is the inhibitor of aurora kinase which is a key enzyme that is implicated in tumor growth .
|
-
- HY-115932
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora kinase-IN-1 (Compound 9) is a potent inhibitor of aurora kinase. Aurora kinase-IN-1 upregulates the expression of G1 cell cycle inhibitory proteins including p21 and p27, and G1 progressive cyclin D1, and downregulates G1-to-S progressive cyclins, resulting in cell cycle arrest at the G1/S boundary. Aurora kinase-IN-1 also induces apoptosis. Aurora kinase-IN-1 is a lead compound for chemotherapeutic agents .
|
-
- HY-176191
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase-IN-7 (compound 4b) is an orally active and selective AURKB inhibitor. Aurora kinase-IN-7 can be used in the study of aggressive cancers .
|
-
- HY-15812
-
|
|
Aurora Kinase
|
Cancer
|
|
XMD-12 (compound 1) is an Aurora kinase (Aurora Kinase) inhibitor with anti-tumor activity that promotes paclitaxel (HY-B0015) induced cell death. XMD-12 exhibits high selectivity and potency against Aurora A, B, and C kinases, with IC50 values of 5.6, 18.4, and 24.6 nM, respectively .
|
-
- HY-170812
-
|
|
Aurora Kinase
|
Cancer
|
|
BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .
|
-
- HY-146037
-
|
|
Apoptosis
Aurora Kinase
|
Cancer
|
|
Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells .
|
-
- HY-121998
-
|
|
Aurora Kinase
|
Others
|
|
Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
|
-
- HY-119951
-
|
|
Aurora Kinase
|
Cancer
|
|
AKI-001 is an prototype pentacyclic inhibitor of aurora kinase with cellular potency of IC50 of less than 100 nM. AKI-001 shows low nanomolar potency against Aurora A and Aurora B enzymes .
|
-
- HY-123279
-
|
|
Aurora Kinase
CDK
|
Cancer
|
|
OM137 is an aurora kinase inhibitor, with an IC50 of 21.7 μM (Aurora A kinase) and 2.4 μM (Aurora B kinase). OM137 also inhibits Cdk1/cyclinB and Cdk5/p25 with an approximate IC50 of 20 μM. OM137 reduces spindle checkpoint-signaling proteins (Mad2 and BubR1) at the kinetochores of chromosomes .
|
-
- HY-10179R
-
|
PHA-739358 (Standard)
|
Reference Standards
Aurora Kinase
Autophagy
|
Cancer
|
|
Danusertib (Standard) is the analytical standard of Danusertib. This product is intended for research and analytical applications. Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
|
-
- HY-156378
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora A inhibitor 3 (Compound 5h) inhibits Aurora-A kinase with an IC50 value of 0.78 μM. Aurora A inhibitor 3 is cytotoxic, with GI50 values of 0.12 μM and 0.63 μM for MCF-7 and MDA-MB-231 cells, respectively .
|
-
- HY-113894
-
|
|
Aurora Kinase
|
Cancer
|
|
Retreversine is an inactive control for Reversine. Reversine is a novel class of ATP-competitive Aurora kinase inhibitor .
|
-
- HY-167114
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
(Rac)-Aurora A/PKC-IN-1 (Compund 2e) is an orally active Aurora A and PKC (α, β1, β2 and θ) kinase inhibitor. (Rac)-Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells in vitro and antimetastatic activity in vivo .
|
-
- HY-W100186
-
|
|
Aurora Kinase
|
Others
|
|
Win 47338 (compound 14) is a control compound of inhibitors of the mitotic kinase monopolar spindle MPS1 and Aurora kinases (AurA/AurB) (Ki>100 μM) .
|
-
- HY-144307
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .
|
-
- HY-164455
-
|
|
STAT
JAK
Aurora Kinase
Mitosis
|
Inflammation/Immunology
|
|
AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
|
-
- HY-10971R
-
|
MLN 8237 (Standard)
|
Aurora Kinase
Autophagy
Apoptosis
Reference Standards
|
Cancer
|
|
Alisertib (Standard) is the analytical standard of Alisertib. This product is intended for research and analytical applications. 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 .
|
-
- HY-10180R
-
|
|
Reference Standards
Aurora Kinase
|
Cancer
|
|
MLN8054 (Standard) is the analytical standard of MLN8054. This product is intended for research and analytical applications. MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
|
-
- HY-123697
-
|
|
Aurora Kinase
|
Cancer
|
|
VE-465 is an Aurora kinase inhibitor. VE-465 induces cancer cell apoptosis. VE-465 has anticancer effects in multiple tumor models .
|
-
- HY-19565
-
|
|
Aurora Kinase
IGF-1R
Apoptosis
|
Cancer
|
|
KW-2450 tosylate is an orally active Aurora A and B kinases, IGF-1R, and IR tyrosine kinases inhibitor. KW-2450 tosylate induces Apoptosis. KW-2450 tosylate also exhibits anticancer activity against triple-negative breast cancer .
|
-
- HY-13072B
-
|
AS-703569 benzoate; R-763 benzoate
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-181082
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase-IN-10 is an Aurora kinase inhibitor. Aurora kinase-IN-10 exhibits IC50 values of 5.94 nM and 86.06 nM against Aurora A and Aurora B, respectively. Aurora kinase-IN-10 has anti-tumor activity and can be used in the research of tumors such as triple-negative breast cancer .
|
-
- HY-183767
-
-
- HY-165369
-
|
|
Aurora Kinase
|
Cancer
|
|
IBPR002 is an inhibitor of Aurora kinase A and Aurora kinase B, with IC50 values of 41 nM and 17 nM, respectively. IBPR002 disrupts the nucleation and bundling of kinetochore microtubules, impairs the bipolarity of mitotic spindles, and promotes the binding of non-phosphorylated hepatoma up-regulated protein (HURP) to microtubules derived from the mother centrosome. IBPR002 reduces tumorigenesis levels in a colorectal cancer xenograft model using athymic nude mice. IBPR002 is applicable for research related to colorectal cancer .
|
-
- HY-181668
-
|
|
ULK
|
Cancer
|
|
ULK1-IN-4 (compound 12i) is a ULK1 inhibitor with an IC50 of 4.7 μM against human ULK1, and it exhibits selectivity for Aurora A/Aurora B kinases. ULK1-IN-4 forms a covalent bond with the thiol group of the Cys182 residue of ULK1, thereby inhibiting the kinase activity of ULK1. ULK1-IN-4 inhibits the growth of colorectal cancer cells and exerts tumor-suppressive activity in a mouse model of colorectal cancer .
|
-
- HY-114526
-
-
- HY-179374
-
|
|
Aurora Kinase
HDAC
Apoptosis
|
Cancer
|
|
Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model .
|
-
- HY-183102
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
ATC12 is a Aurora-A kinase inhibitor. ATC12 binds to Aurora-A and competes with TPX2 for binding to disrupt the Aurora-A/TPX2 interaction. ATC12 inhibits cancer cell proliferation, induces apoptosis and cellular senescence. ATC12 can be used in the research of breast cancer .
|
-
- HY-10128R
-
|
|
Aurora Kinase
Reference Standards
Apoptosis
|
Cancer
|
|
ZM-447439 (Standard) is the analytical standard of ZM-447439 (HY-10128). This product is intended for research and analytical applications. ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively.
|
-
- HY-10329R
-
|
|
Reference Standards
Aurora Kinase
CDK
Apoptosis
|
Cancer
|
|
JNJ-7706621 (Standard) is the analytical standard of JNJ-7706621 (HY-10329). This product is intended for research and analytical applications. 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 .
|
-
- HY-10339R
-
|
|
Reference Standards
FLT3
FGFR
Bcr-Abl
Aurora Kinase
Apoptosis
|
Cancer
|
|
KW-2449 (Standard) is the analytical standard of KW-2449 (HY-10339). This product is intended for research and analytical applications. KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
|
-
- HY-183960
-
|
|
ASK1
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
BPyO-34 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 0.52 μM against human targets. BPyO-34 inhibits the activity of ASK1 in in vitro kinase assays. BPyO-34 can be used in research related to various diseases such as diabetes and cancer .
|
-
- HY-10161R
-
|
VX 680 (Standard); MK-0457 (Standard)
|
Aurora Kinase
Reference Standards
Autophagy
|
Cancer
|
|
Tozasertib (Standard) is the analytical standard of Tozasertib (HY-10161). This product is intended for research and analytical applications. Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.
|
-
- HY-104023
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
ZK-Thiazolidinone is an ATP-competitive Polo-like kinase 1 (Plk1) inhibitor with an IC50 of 19 nM. ZK-Thiazolidinone inhibits tumor cell proliferation, induces cell cycle arrest and typical mitotic defects. ZK-Thiazolidinone impairs the recruitment of γ-tubulin and Aurora A kinase to centrosomes, resulting in failure of bipolar spindle maintenance and sister chromatid arm cohesion.\nZK-Thiazolidinone is applicable for cancer research .
|
-
- HY-181568
-
|
|
PROTACs
Aurora Kinase
DNA/RNA Synthesis
Apoptosis
|
Neurological Disease
Cancer
|
|
PROTAC Aurora A Degrader-1 (Compound 280) is a blood-brain barrier-permeable selective Aurora A PROTAC degrader, with DC50 values of 1 nM and 2 nM in LAN5 and SMS-SAN cells, respectively. PROTAC Aurora A Degrader-1 induces the formation of a ternary complex between AURKA and CRBN, degrades AURKA, reduces MYCN levels, induces DNA damage and apoptosis, exerts antiproliferative activity in cancer cells, and regulates the immune system. PROTAC Aurora A Degrader-1 is applicable to the research of neuroblastoma and small cell lung cancer .
|
-
- HY-181275
-
|
|
Ligands for Target Protein for PROTAC
CDK
HIV
|
Infection
|
|
CDK9 ligand 4 is a CDK9 ligand. As a ligand for target protein for PROTAC (Ligands for Target Protein for PROTAC), CDK9 ligand 4 serves for the development and design of PROTAC CDK9 degraders, such as PROTAC CDK9 degrader-12 (HY-181231). CDK9 ligand 4 is applicable to the research of HIV-1 infection .
|
-
- HY-119618
-
|
|
Endogenous Metabolite
|
Cancer
|
|
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
|
-
- HY-10058
-
|
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
|
AT9283 lactic acid 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 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo .
|
-
- HY-18955
-
|
|
MEK
Aurora Kinase
Apoptosis
|
Cancer
|
|
BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. BI-847325 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-13072R
-
|
AS-703569 (Standard); R-763 (Standard)
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
Reference Standards
|
Cancer
|
|
Cenisertib (Standard) is the analytical standard of Cenisertib. This product is intended for research and analytical applications. Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-10987A
-
|
|
Aurora Kinase
FLT3
VEGFR
FGFR
PDGFR
Src
Apoptosis
|
Cancer
|
|
ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
|
-
- HY-114302
-
CCB02
1 Publications Verification
|
Microtubule/Tubulin
|
Cancer
|
|
CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1 .
|
-
- HY-12564
-
|
|
Aurora Kinase
Apoptosis
Mitosis
|
Cancer
|
|
Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells .
|
-
- HY-10987
-
|
|
Aurora Kinase
FLT3
VEGFR
FGFR
Src
PDGFR
Apoptosis
|
Cancer
|
|
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
|
-
- HY-125158
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
HOI-07 is a selective Aurora B kinase inhibitor. HOI-07 blocks phosphorylation of histone H3 on Ser10 in
lung cancer cells. HOI-07 induces cell-cycle arrest, and apoptosis. HOI-07 has antitumor activity, and suppresses the tumor growth of A549, 143B and KHOS xenografts .
|
-
- HY-116423A
-
|
|
NEKs
|
Cancer
|
|
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-116423
-
|
|
NEKs
|
Cancer
|
|
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15720B
-
|
|
ROCK
Aurora Kinase
CaMK
|
Neurological Disease
|
|
Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC50s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride .
|
-
- HY-162470
-
|
|
Aurora Kinase
|
Cancer
|
|
DBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465 .
|
-
- HY-114258
-
|
AK-01
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
LY3295668 (AK-01) is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki 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 .
|
-
- HY-182391
-
|
|
MASTL
Apoptosis
Aurora Kinase
PARP
Caspase
|
Cancer
|
|
MKI-3 is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC50 of 5.72 nM and a Kd 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 .
|
-
- HY-181311
-
|
|
PROTACs
Aurora Kinase
E1/E2/E3 Enzyme
|
Neurological Disease
Cancer
|
|
CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma .
|
-
- HY-175982
-
|
|
Aurora Kinase
|
Cancer
|
|
AURKA-IN-3 (Compound AL8) is an irreversible covalent Aurora kinase A (AURKA) inhibitor with an IC50 value of 23.0 nM. AURKA-IN-3 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by AURKA, and reduces the autophosphorylation level of AURKA. AURKA-IN-3 is promising for research of malignant tumors associated with high AURKA expression (e.g., leukemia, lymphoma) .
|
-
- HY-168022
-
CAM2602
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
CAM2602 is an orally active Aurora A-TPX2 protein−protein interaction inhibitor with a human Kd of 19 nM for Aurora A. CAM2602 increases the proportion of PH3 positive cells while reducing P-T288 Aurora A levels. CAM2602 arrests tumor xenograft growth in mice. CAM2602 can be used for the research of cancer, such as acute T cell leukemia .
|
-
- HY-114258A
-
|
AK-01 erbumine
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
LY3295668 (AK-01) erbumine is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 erbumine can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 erbumine avoids the formation of polyploids related to AurB inhibition. LY3295668 erbumine can be used for the study of small cell lung cancer .
|
-
- HY-50514R
-
|
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
|
AT9283 (Standard) is the analytical standard of AT9283. This product is intended for research and analytical applications. 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 .
|
-
- HY-W395613
-
|
|
Aurora Kinase
|
Cancer
|
|
TY-011 is an Aurora A/B kinase inhibitor. TY-011 induces abnormal microtubule-kinetochore attachment, leading to DNA damage and apoptosis (Apoptosis) in human gastric cancer cells, and ultimately inhibits cancer cell proliferation, with an IC50 value ranging from 0.11 to 4.49 μM in human gastric cancer cell lines. TY-011 has potential applications in gastric cancer research .
|
-
- HY-125090
-
|
|
Aurora Kinase
c-Myc
Bcr-Abl
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells .
|
-
- HY-157396
-
|
|
Aurora Kinase
Apoptosis
Caspase
|
Cancer
|
|
JAB-2485 is an orally active and selective Aurora kinase A (AURKA) inhibitor with an IC50 value of 0.327 nM. JAB-2485 exhibits inhibitory activity against various tumor cell lines such as neuroblastoma, triple-negative breast cancer, small cell lung cancer, and epithelial ovarian cancer. JAB-2485 can induce cell cycle arrest and apoptosis in tumor cells. JAB-2485 has antitumor activity .
|
-
- HY-123919
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib?(HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984) .
|
-
- HY-122582
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984) .
|
-
- HY-115862
-
|
|
Adenosine Receptor
PARP
Aurora Kinase
|
Cardiovascular Disease
Cancer
|
|
Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM .
|
-
- HY-10320G
-
|
BIRB 796 (GMP)
|
p38 MAPK
|
Cancer
|
|
Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity .
|
-
- HY-173499
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies) .
|
-
- HY-175525
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors (Pink: Target protein ligand (HY-175526); Blue: E3 ligand (HY-112078); Black: Linker; E3 ligand + Linker (HY-132938)) .
|
-
- HY-167854
-
|
|
Aurora Kinase
Apoptosis
IGF-1R
|
Cancer
|
|
KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
|
-
- HY-N0419
-
|
Quercetin-7-O-β-D-glucopyranoside
|
Glycosidase
c-Kit
MMP
VEGFR
Aurora Kinase
|
Metabolic Disease
Cancer
|
|
Quercimeritrin (Quercetin-7-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor (with an IC50 of 79.88 μM against the Saccharomyces cerevisiae enzyme) and a P-gp substrate, with anti-angiogenic and antioxidant activities. Quercimeritrin does not cross the blood-brain barrier and does not inhibit cytochrome P450 enzymes. Quercimeritrin precisely binds to and inhibits the active sites of c-Kit, MMP-2, Aurora-A kinases and α-glucosidase, thereby disrupting target functions. Quercimeritrin effectively regulates postprandial blood glucose and also exhibits significant anti-angiogenic activity, which inhibits endothelial cell proliferation and microvascular growth. Quercimeritrin can be used in the research of diabetes and breast cancer .
|
-
-
-
HY-L004
-
|
|
3,313 compounds
|
|
DNA is prone to numerous forms of damage that can injure cells and impair fitness. Cells have developed an array of mechanisms to repair these injuries. Proliferating cells are especially vulnerable to DNA damage due to the added demands of cellular growth and division. Cell cycle checkpoints represent integral components of DNA repair that coordinate cooperation between the machinery of the cell cycle and several biochemical pathways that respond to damage and restore DNA structure. By delaying progression through the cell cycle, checkpoints provide more time for repair before the critical phases of DNA replication, when the genome is replicated, and of mitosis, when the genome is segregated. Loss or attenuation of checkpoint function may increase spontaneous and induced gene mutations and chromosomal aberrations by reducing the efficiency of DNA repair.
MCE owns a unique collection of 3,313 cell cycle/DNA damage-related compounds which can be used in the research of the same.
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0419
-
-
-
- HY-N3737
-
-
-
- HY-N3634
-
|
|
Leguminosae
Phenols
Polyphenols
Psoralea corylifolia L.
Plants
Source Classification
|
EGFR
TAM Receptor
Tie
|
|
Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-116423
-
|
|
|
Alkynes
|
|
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-175827
-
|
|
|
Alkynes
|
|
MK-5108-NH-PEG2-alkyne is a Aurora kinase A (AURKA) inhibitor. MK-5108-NH-PEG2-alkyne can be used for synthesis of PROTAC AURKA degrader 1 (HY-175830) .
|
-
- HY-116423A
-
|
|
|
Alkynes
|
|
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: