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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
45 Results for "
Aurora-A
" in MedChemExpress (MCE) Product Catalog:
Products (45)
45 Results for "Aurora-A" in MCE Product Catalog:
4
4 Cited Publications
Target:
Research Areas:
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 .
4
Target:
Checkpoint Kinase (Chk) VEGFR Src c-Fms Aurora Kinase FGFR FLT3 RET CDK
Research Areas:
PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
3
Target:
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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 .
3
3 Cited Publications
Target:
Research Areas:
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 .
3
3 Cited Publications
Research Areas:
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 .
2
2 Cited Publications
Synonyms: Quercetin-7-O-β-D-glucopyranoside
Category:
Flavonols Ginkgoaceae Metabolic Disease Plants Compositae Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids Derris scandens Ginkgo biloba L. Disease Research Fields
Target:
1
Target:
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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 .
1
1 Cited Publications
Research Areas:
GRK2 Inhibitor 2 is an orally active and selective G protein-coupled receptor kinase 2 (GRK) inhibitor with an IC50 of 19 nM. GRK2 Inhibitor 2 also inhibits Aurora-A with an IC50 of 137 nM. GRK2 Inhibitor 2 can be used in the study of congestive heart failure (HF) .
Cat. No.: HY-18161
CAS No.: 1402709-93-6
Target:
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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).
Cat. No.: HY-168439
CAS No.: 2566733-45-5
Target:
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HLB-0532259 is a Aurora-A/N-Myc PROTAC degrader, with a DC50 of 20.2 nM against Aurora-A in MCF-7 cells; its DC50 values against N-Myc are 179 nM in SK-N-BE (2) cells and 229 nM in Kelly cells, respectively. HLB-0532259 induces apoptosis (apoptosis) in MYCN-amplified neuroblastoma cells and inhibits tumor growth in mouse xenograft models. HLB-0532259 can be used for the research of neuroblastoma .
Cat. No.: HY-W002016
CAS No.: 253-52-1
Target:
Research Areas:
Cardiovascular Disease Infection Metabolic Disease Inflammation/Immunology Cancer
Phthalazine is a chemical scaffold. Phthalazine derivatives act as VEGFR-2 inhibitors, PARP-1 inhibitors, and anticancer agents. The complex of phthalazine with silver exhibits broad-spectrum antibacterial and antifungal activities against Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa PAO1, and Candida albicans. Phthalazine derivatives possess potent vasodilatory activity. Phthalazine can be used in research related to colon adenocarcinoma, breast cancer, hypertension, diabetes, and microbial infections .
Cat. No.: HY-168440
CAS No.: 2541626-73-5
Research Areas:
Aurora-A ligand 1 is a high-affinity and specific Aurora-A inhibitor with a dissociation constant (Kd) value of 0.85 nM. Aurora-A ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC Aurora-A degraders with antitumor activity. Aurora-A ligand 1 can be used for the synthesis of HLB-0532259 (HY-168439). HLB-0532259 shows anti-tumor activity against neuroblastoma .
Target:
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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 .
Cat. No.: HY-171770
CAS No.: 3115765-45-9
Research Areas:
dAurAB5 is a dual Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236) .
Cat. No.: HY-171769
CAS No.: 3115765-38-0
Target:
Research Areas:
dAurAB2 is a dual-degrading PROTAC that potently degrades Aurora-A and Aurora-B with DC50s of 59 nM and 39 nM, respectively. dAurAB2 reduces N-Myc levels in MYCN-amplified IMR32 neuroblastoma cells. dAurAB2 can be used for the study of neuroblastoma. (Pink, Aurora ligand (HY-10804); Blue, E3 ligand: (HY-103597); Black, linker (HY-W105740)) .
Research Areas:
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM .
Target:
Research Areas:
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 .
Cat. No.: HY-W231513
CAS No.: 321945-24-8
Target:
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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 .
Cat. No.: HY-178343
Target:
Research Areas:
Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
