Search Result
Results for "
dual kinase inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-114332
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- HY-132893
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TAM Receptor
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Cancer
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AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
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- HY-101053
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Src kinase inhibitor 1; Src-l1
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Src
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Cancer
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Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
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- HY-77251
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MAP4K
MAP3K
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Cancer
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TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
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- HY-178163
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Ferroptosis
Necroptosis
RIP kinase
Reactive Oxygen Species (ROS)
Mixed Lineage Kinase
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Inflammation/Immunology
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Zharp1-163 is a dual inhibitor of ferroptosis and necroptosis. Zharp1-163 effectively blocks ferroptosis by reducing reactive oxygen species (ROS) levels and inhibits necroptosis by potently and selectively targeting RIPK1 kinase activity (KD = 240 nM; IC50 = 406.1 nM). Zharp1-163 inhibits the cellular activation of RIPK1, RIPK3 and MLKL in response to necroptotic stimulation. Zharp1-163 markedly attenuates TNF-α (HY-P1875)-induced systemic inflammatory syndrome, including the prevention of TNF-α-induced mortality and hypothermia in mice. Zharp1-163 significantly alleviates acute kidney injury associated with both necroptosis and ferroptosis in models induced by Cisplatin (HY-17394) and ischemia-reperfusion. Zharp1-163 can be used for the study of diseases associated with cell death pathways, such as kidney disease .
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- HY-15496
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ER-806201
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MEK
FLT3
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Cancer
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E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
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- HY-144438
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Aurora Kinase
LIM Kinase (LIMK)
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Cancer
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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 .
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- HY-160172A
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- HY-160172
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- HY-147703
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Aurora Kinase
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Cancer
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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 .
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- HY-141864
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Itk
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Inflammation/Immunology
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ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
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- HY-10460
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Pyk2
FAK
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Cancer
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PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively .
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- HY-108709
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CC-671
1 Publications Verification
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CDK
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Cancer
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CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively.
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- HY-162952
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Bcr-Abl
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Cancer
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cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target cSRC/BCR-ABL1 kinase inhibitor .
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- HY-13068
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E-7050
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c-Met/HGFR
VEGFR
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Cancer
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Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
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- HY-101798
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PI3K
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Cancer
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MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .
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- HY-13455
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Haspin Kinase
DYRK
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Cancer
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LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively .
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- HY-13455A
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Haspin Kinase
DYRK
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Cancer
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LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively .
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- HY-N12625
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CDK
DYRK
GSK-3
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Cancer
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(R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC50s of 1.1, 0.95, >10, >10 and >10 μM, respectively .
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- HY-153120A
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PI3K
mTOR
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Cancer
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PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
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- HY-153120
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PI3K
mTOR
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Cancer
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PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
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- HY-10181S
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BMS-354825-d8
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Bcr-Abl
Src
Apoptosis
Autophagy
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Cancer
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Dasatinib-d8 (BMS-354825-d8) is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.
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- HY-18161
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FLT3
Aurora Kinase
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Cancer
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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).
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- HY-112314
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Src
Bcr-Abl
Apoptosis
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Cancer
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AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity . AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells .
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- HY-108606
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PI-828
2 Publications Verification
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PI3K
Casein Kinase
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Cancer
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PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively .
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- HY-170812
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Aurora Kinase
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Cancer
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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 .
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- HY-12299
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dual LCK/SRC inhibitor
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Src
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Cancer
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WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
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- HY-131669
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Dasatinib carboxylic acid
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Drug Metabolite
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Others
Cancer
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Dasatinib metabolite M6 (Dasatinib carboxylic acid) is an oxidative metabolite of Dasatinib (HY-10181). Dasatinib is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor .
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- HY-N12041
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TAM Receptor
HIF/HIF Prolyl-Hydroxylase
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Cancer
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Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression .
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- HY-16962A
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DNA-PK
mTOR
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Cancer
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CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
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- HY-16962
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CC-115
2 Publications Verification
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DNA-PK
mTOR
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Cancer
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CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
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- HY-160685
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VEGFR
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Others
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GW809897X is a dual inhibitor of Fluc and VEGFR with IC50 of 0.58 μM and 65 nM, respectively. GW809897X is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential impact on Fluc reporter assays .
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- HY-160684
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VEGFR
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Others
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GW701427A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.12 μM and 603 nM, respectively. GW701427A acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays .
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- HY-112273A
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Aurora Kinase
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Cancer
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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 .
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- HY-112273
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CD532
1 Publications Verification
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Aurora Kinase
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Cancer
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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 .
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- HY-19642
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MGCD265
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TAM Receptor
c-Met/HGFR
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Cancer
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Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
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- HY-19642A
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MGCD265 hydrochloride
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TAM Receptor
c-Met/HGFR
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Cancer
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Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
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- HY-158975
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Casein Kinase
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Cancer
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VRK1/CK1-IN-1 (compound 36) is a dual inhibitor of vaccinia-related kinase 1 (VRK1) and casein kinase 1 (CK1), with the Ki of 37.9 nM for VRK1 and IC50s of 17 nM and 15 nM for δ and ε isoforms of CK1, respectively .
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- HY-100398
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PI3K
mTOR
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Cancer
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PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
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- HY-N0737A
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- HY-101549A
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UNC2371 hydrochloride
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FLT3
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Cancer
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MRX-2843 hydrochloride is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
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- HY-147243
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ANG-3070
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VEGFR
PDGFR
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Cardiovascular Disease
Inflammation/Immunology
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Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases .
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- HY-10412
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KT7515
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JNK
Mixed Lineage Kinase
MDM-2/p53
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Neurological Disease
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CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53 .
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- HY-148233S
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Casein Kinase
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Others
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JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure .
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- HY-13068R
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c-Met/HGFR
VEGFR
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Cancer
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Golvatinib (Standard) is the analytical standard of Golvatinib. This product is intended for research and analytical applications. Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
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- HY-117273
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Raf
Autophagy
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Cancer
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AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity .
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- HY-12947
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MAP3K
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Neurological Disease
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GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases .
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- HY-101549
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UNC2371
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FLT3
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Cancer
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MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
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- HY-15174
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BEZ235 Tosylate; NVP-BEZ 235 Tosylate
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PI3K
mTOR
Autophagy
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Cancer
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Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
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- HY-13838
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c-Fms
c-Kit
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Cancer
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PLX647 is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively) .
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- HY-13838A
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c-Fms
c-Kit
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Inflammation/Immunology
Cancer
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PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively) .
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- HY-12572
-
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Tie
VEGFR
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Cancer
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TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively . TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research .
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- HY-W011266
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PDGFR
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Cancer
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JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
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- HY-128758
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DYRK
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Cancer
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DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity .
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- HY-128758A
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DYRK
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Cancer
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DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity .
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- HY-156423
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Microtubule/Tubulin
JAK
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Cancer
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Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells .
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- HY-114356
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c-Met/HGFR
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Cancer
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BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma .
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- HY-164455
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STAT
JAK
Aurora Kinase
Mitosis
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Inflammation/Immunology
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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) .
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- HY-112708
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PF-06700841
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JAK
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Inflammation/Immunology
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Brepocitinib (PF-06700841) is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively .
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- HY-12680
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PRN694
2 Publications Verification
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Itk
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Inflammation/Immunology
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PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo .
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- HY-128677
-
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Casein Kinase
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Neurological Disease
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NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms .
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- HY-174134
-
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PI4K
PKG
Parasite
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Infection
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PI4Kβ/PKG-IN-2 (Compound 20) is an orally active dual inhibitor of Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-2 has potent inhibitory effects on Plasmodium. PI4Kβ/PKG-IN-2 is promising for research of malaria .
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- HY-174130
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Parasite
PI4K
PKG
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Infection
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PI4Kβ/PKG-IN-1 (Compound 19) is an orally active dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-1 exhibits potent antiplasmodial activity. PI4Kβ/PKG-IN-1 is promising for research of malaria .
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- HY-116191
-
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PI3K
mTOR
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Cancer
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WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
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- HY-164454
-
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Aurora Kinase
STAT
JAK
Mitosis
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Inflammation/Immunology
|
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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) .
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- HY-160686
-
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VEGFR
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Others
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GSK248233A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 1.03 μM and 2 nM, respectively. GSK248233A also shows activity against the AGC family. GSK248233A acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays .
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- HY-112708A
-
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PF-06700841 P-Tosylate
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JAK
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Inflammation/Immunology
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Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively .
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- HY-162143
-
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SphK
Akt
mTOR
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Cancer
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SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells .
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- HY-19383
-
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PTP 112
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Phosphatase
IKK
PPAR
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Metabolic Disease
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Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
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- HY-100867
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TAK-659; CB-659
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Syk
FLT3
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Cancer
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TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
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- HY-176410
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IRAK
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Cancer
|
|
IRAK1/4/pan-FLT3 Kinase-IN-2 (compound 27) is a potent IRAK1/4 and FLT3 dual inhibitor with IC50s of 10, 0.7, and <0.5 nM. IRAK1/4/pan-FLT3 Kinase-IN-2 extends acute myeloid leukemia model mouse survival .
|
-
- HY-100867A
-
|
TAK-659 monohydrochloride; CB-659 monohydrochloride
|
Syk
FLT3
|
Cancer
|
|
TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-14243
-
|
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
VEGFR
Tie
|
Cancer
|
|
CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC50 value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma .
|
-
- HY-15841
-
|
|
Anaplastic lymphoma kinase (ALK)
FAK
|
Cancer
|
|
CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397) .
|
-
- HY-179031
-
|
|
EGFR
VEGFR
Apoptosis
|
Cancer
|
|
EGFR/VEGFR2-IN-7 (Compound 3e) is a dual-target EGFR/VEGFR2 inhibitor, with IC50 values of 142 (EGFR) and 71 nM (VEGFR2). EGFR/VEGFR2-IN-7 exhibits broad-spectrum and potent anti-proliferative activity, especially being sensitive to breast cancer. EGFR/VEGFR2-IN-7 induces cell cycle arrest and apoptosis, inhibits cell migration and invasion. EGFR/VEGFR2-IN-7 can be used for research on breast cancer .
|
-
- HY-114205A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
|
-
- HY-161351
-
|
|
Akt
STAT
Apoptosis
|
Cancer
|
|
STAT3/AKT-IN-1 is a dual inhibitor for the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signalling pathway, exhibits antitumor activity against gastric cancer and induces cell apoptosis in SGC-7901 cells .
|
-
- HY-114205
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
|
-
- HY-15838
-
ID-8
5 Publications Verification
|
DYRK
|
Cancer
|
|
ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs .
|
-
- HY-12279
-
|
TGR-1202; RP5264
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach .
|
-
- HY-12279A
-
|
TGR-1202 tosylate; RP5264 tosylate
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach .
|
-
- HY-12279C
-
|
TGR-1202 hydrochloride; RP5264 hydrochloride
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach .
|
-
- HY-149874
-
|
|
DGK
|
Inflammation/Immunology
Cancer
|
|
BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research .
|
-
- HY-151211
-
|
|
Btk
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia .
|
-
- HY-136310
-
|
|
PI5P4K
|
Cancer
|
|
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways .
|
-
- HY-152142
-
|
|
JNK
|
Neurological Disease
|
|
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability .
|
-
- HY-12279B
-
|
TGR-1202 sulfate; RP-5264 sulfate
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach .
|
-
- HY-N0737AR
-
|
Telepathine (Standard)
|
Reference Standards
DYRK
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
|
-
- HY-19322B
-
|
LGH447 dihydrochloride
|
Pim
Apoptosis
|
Cancer
|
|
PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis .
|
-
- HY-148629
-
|
|
JNK
|
Neurological Disease
|
|
GDC-0134 is a potent, selective, orally active, brain-penetrant dual leucine zipper kinase (DLK) inhibitor. GDC-0134 blocks DLK activity in cellular assays and in animal models of neuronal injury. GDC-0134 can be used for the study of amyotrophic lateral sclerosis (ALS) .
|
-
- HY-19322
-
|
LGH447
|
Pim
Apoptosis
|
Cancer
|
|
PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis .
|
-
- HY-13737
-
R1530
1 Publications Verification
|
Apoptosis
VEGFR
FGFR
Mitosis
|
Cancer
|
|
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence .
|
-
- HY-103439
-
|
|
EGFR
|
Cancer
|
|
GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity .
|
-
- HY-15174R
-
|
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
Dactolisib (Tosylate) (Standard) is the analytical standard of Dactolisib (Tosylate). This product is intended for research and analytical applications. Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
|
-
- HY-179022
-
|
|
Carbonic Anhydrase
CDK
Apoptosis
|
Cancer
|
|
CAIX/CDK-2-IN-1 is a dual-acting inhibitor of carbonic anhydrase IX (CA IX) and cyclin-dependent kinase-2 (CDK-2) with IC50 values of 0.29 μM and 0.32 μM. The zein nanoparticls of CAIX/CDK-2-IN-1 can induce cancer cells apoptosis. CAIX/CDK-2-IN-1 can be used for the research of cancer, such as ling cancer .
|
-
- HY-128142
-
|
|
PKD
PKC
|
Cardiovascular Disease
|
|
PKC/PKD-IN-1 (Compound 13C) is an orally active dual protein kinase C/D (PKC/PKD) inhibitor with an IC50 value of 0.6 nM for PKD1. PKC/PKD-IN-1 can attenuate high-salt diet-induced cardiac hypertrophy and can be used in the study of heart failure .
|
-
- HY-117049
-
|
|
DYRK
CDK
GSK-3
Apoptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
Metabolic Disease
|
|
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) and CDC-like kinases (CLKs). Leucettine L41 can also inhibit GSK-3 singnaling. Leucettine L41 can inhibit cell apoptosis and ROS production. Leucettine L41 can promote β-cell cell cycle progression, cell proliferation and increase insulin secretion. Leucettine L41 can be used for the researches of neurological disease and metabolic disease, such as Alzheimer’s disease (AD) and diabetes .
|
-
- HY-145723
-
|
|
FLT3
FGFR
|
Inflammation/Immunology
Cancer
|
|
MAX-40279 is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 is also effective against the FLT3 mutants such as FLT3 D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 can be used for the research of acute myelogenous leukemia (AML) .
|
-
- HY-145723A
-
|
|
FLT3
FGFR
|
Inflammation/Immunology
Cancer
|
|
MAX-40279 hydrochloride is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hydrochloride is also effective against the FLT3 mutants such as FLT3 D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 hydrochloride inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hydrochloride can be used for the research of acute myelogenous leukemia (AML) .
|
-
- HY-160687
-
|
|
VEGFR
|
Others
|
|
GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.26 μM and 1.2 μM, respectively. GW549390X can bind to the ATP pocket of FLuc through the aniline side chain and is an ATP-competitive inhibitor of Fluc. GW549390X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, with potential implications for Fluc reporter assays .
|
-
- HY-170484
-
|
|
MAP3K
p38 MAPK
|
Neurological Disease
|
|
KAI-11101 is the inhibitor for dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. KAI-11101 inhibits Paclitaxel (HY-B0015)-induced cJun phosphorylation (IC50=95 nM) and thus inhibits the activation of MAPK pathway. KAI-11101 is blood brain barrier penetrable and can be further investigated for its neuroprotective property .
|
-
- HY-148868
-
|
|
Akt
PKA
CDK
|
Others
|
|
Akt1&PKA-IN-1 is a potent dual Akt/PKA inhibitor with IC50 values of 0.03 , 0.11 μM, and 9.8 μM for PKAa, Akt, and CDK2, respectively. Akt1&PKA-IN-1 is selective for cyclin-dependent kinase 2 (CDK2) .
|
-
- 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-12279CR
-
|
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (hydrochloride) (Standard) is the analytical standard of Umbralisib (hydrochloride). This product is intended for research and analytical applications. Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach .
|
-
- HY-12279R
-
|
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (Standard) is the analytical standard of Umbralisib. This product is intended for research and analytical applications. Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach .
|
-
- HY-145723C
-
|
|
FLT3
FGFR
|
Inflammation/Immunology
Cancer
|
|
MAX-40279 hemiadipate is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemiadipate is also effective against the FLT3 mutants such as FLT3 D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 hemiadipate inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemiadipate can be used for the research of acute myelogenous leukemia (AML) .
|
-
- HY-145723B
-
|
|
FLT3
FGFR
|
Inflammation/Immunology
Cancer
|
|
MAX-40279 hemifumarate is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemifumarate is also effective against the FLT3 mutants such as FLT3 D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 hemifumarate inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemifumarate can be used for the research of acute myelogenous leukemia (AML) .
|
-
- HY-13299
-
MK-8033
2 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-13299A
-
|
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-156872
-
|
|
PI3K
EGFR
Syk
Apoptosis
|
Cancer
|
|
MTX-216 is a dual ATP-competitive inhibitor of PI3K and EGFR. MTX-216 cosuppresses Ki-67 and ribosomal S6 phosphorylation and induces apoptosis in NF1 LOF cells. MTX-216 suppresses the activity of SYK kinase, with an IC50 of 281 nM. MTX-216 is used in the research of Melanoma .
|
-
- HY-114331
-
|
|
MAP3K
FLT3
PAK
STK33
Trk Receptor
|
Neurological Disease
|
|
DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a Ki value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research .
|
-
- HY-124645
-
|
|
Flavivirus
Dengue Virus
Btk
MNK
|
Infection
Cancer
|
|
QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC50s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti-dengue virus 2 activity, with an IC50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies .
|
-
- HY-10811
-
GNE-493
2 Publications Verification
|
PI3K
mTOR
|
Cancer
|
|
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
|
-
- HY-155151
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK2/3-IN-1 is a potent dual RIPK2/3 kinases inhibitor with IC50 values of 3 nM and 117 nM, respectively. RIPK2/3-IN-1 is against RIPK2 with IC50 value 14 nM in 14-TriLAN-Gly/NOD1 THP-1 cell-based NF-κB reporter assay .
|
-
- 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-160557
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
PLK1/BRD4-IN-2 (compound 15) is a BI-2536 (HY-50698) analog and dual inhibitor that targets both Polo-like kinase 1 (PLK1) and BRD4bromodomain (BRD4-BD1 IC50=28 nM, PLK1 IC50=40 nM) .
|
-
- HY-176561
-
|
|
Casein Kinase
HDAC
|
Cancer
|
|
IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research .
|
-
- HY-N0737AG
-
|
Telepathine
|
DYRK
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
|
-
- HY-147992
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-147994
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-160558
-
|
|
Epigenetic Reader Domain
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC50s of 0.059, 0.127 and 0.245 μM, respectively .
|
-
- HY-123468
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-123468A
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-10424
-
|
PHA-848125
|
CDK
Autophagy
|
Cancer
|
|
Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
|
-
- HY-146492
-
|
|
VEGFR
Raf
Apoptosis
|
Cancer
|
|
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase .
|
-
- HY-147060
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease .
|
-
- HY-103018
-
|
ASN-002
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
|
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
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- HY-15268
-
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c-Met/HGFR
PI3K
DNA-PK
mTOR
Bcr-Abl
Src
VEGFR
EGFR
PDGFR
|
Cancer
|
|
PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research .
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- HY-103018A
-
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ASN-002 hydrochloride
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JAK
Syk
|
Inflammation/Immunology
Cancer
|
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Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
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- HY-50673
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Dactolisib
Maximum Cited Publications
63 Publications Verification
BEZ235; NVP-BEZ235
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PI3K
mTOR
Autophagy
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Cancer
|
|
Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
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- HY-162645
-
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TAM Receptor
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Inflammation/Immunology
Cancer
|
|
BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
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- HY-W007977
-
|
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Drug Intermediate
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Cancer
|
|
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline (Compound 11 and 15) is a building block and synthetic intermediate, which can be used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histone deacetylase (HDAC) inhibitors, and anticancer agents. 4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline can also be used to synthesize EGFR inhibitors, including Erlotinib (HY-50896), with antiproliferative activity .
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- HY-135906
-
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Casein Kinase
ERK
Pim
DYRK
Apoptosis
|
Cancer
|
|
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy .
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- HY-112348
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Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
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-
- HY-10620
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer .
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-
- HY-146491
-
|
|
VEGFR
Raf
Apoptosis
|
Cancer
|
|
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase .
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-
- HY-128879
-
|
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Phosphodiesterase (PDE)
GSK-3
|
Neurological Disease
|
|
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS) .
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-
- HY-128879A
-
|
|
Phosphodiesterase (PDE)
GSK-3
|
Neurological Disease
|
|
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS) .
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-
- HY-173298
-
|
|
PDHK
|
Inflammation/Immunology
Cancer
|
|
PDHK1-IN-2 (Compound 24) is an ATP-competitive dual inhibitor of pyruvate dehydrogenase kinases 1/2 (PDHK1/2), with an IC50 of 0.007 μM for PDHK1 and an IC50 of 0.015 μM for PDHK2. PDHK1-IN-2 can regulate immune cell metabolism and correct mitochondrial dysfunction, and is expected to be used in the research of autoimmune diseases, inflammatory diseases, cancers, and other conditions .
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-
- HY-175479
-
|
|
Salt-inducible Kinase (SIK)
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
GLPG4970 is a potent, selective and orally active salt-inducible kinase 2/3 (SIK2/SIK3) dual inhibitor with IC50 values of 0.3 nM and 0.7 nM. GLPG4970 has weak inhibition of hERG channel with an IC50 of 29 μM. GLPG4970 can decrease TNFα release and increase IL-10 release GLPG4970 can be used for the researches of inflammation and immunology, such as colitis .
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-
- HY-111164
-
|
|
p38 MAPK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CBS-3595 is a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 with anti-inflammatory and anti-allodynic activities. CBS-3595 reduces the production of the proinflammatory cytokine IL-6 and increases the levels of the anti-inflammatory cytokine IL-10 in rats. CBS-3595 reduces paw oedema formation in the Complete Freund’s adjuvant (CFA) (HY-153808)-induced arthritis rat model. CBS-3595 is promising for research of autoimmune diseases .
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-
- HY-149667
-
|
|
DGK
|
Cancer
|
|
BMS-332 is a dual DGKα/ζ lipid kinase inhibitor, with IC50s of 5 and 1 nM against DGKα and DGKζ, respectively. BMS-332 enhances the antigen-specific T cell response. BMS-332 reduces the viral load in the liver and spleen when combined with anti-PD-1 in chronic infection models. BMS-332 can be used for the study of T cell immune checkpoint strategy .
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-
- HY-10424R
-
|
PHA-848125 (Standard)
|
Reference Standards
CDK
Autophagy
|
Cancer
|
|
Milciclib (Standard) is the analytical standard of Milciclib. This product is intended for research and analytical applications. Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
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-
- HY-170940
-
|
|
DYRK
Enterovirus
|
Infection
|
|
Dyrk1A-IN-12 (compound S43) is a Dyrk (Dual specificity tyrosine phosphorylation regulated kinase 1A inhibitor. Dyrk1A-IN-12 inhibits Dyrk1A with a IC50 of 95 nM. Dyrk1A-IN-12 shows anti-EV-A71 activity with an EC50 of 4.4 μM, CC50 of 12.8 μM and SI of 2.9. Dyrk1A-IN-12 shows potent inhibition against herpes simplex virus (HSV) .
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-
- HY-101034
-
|
CHMFL-ABL-KIT-155
|
Bcr-Abl
c-Kit
Apoptosis
PDGFR
Discoidin Domain Receptor
|
Cancer
|
|
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .
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-
- HY-169075
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
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-
- HY-108543
-
|
|
Phosphatase
Apoptosis
|
Cancer
|
|
NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)) . NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway .
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-
- HY-150537
-
|
|
Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
|
Neurological Disease
|
|
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
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-
- 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 .
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-
- HY-161667
-
|
|
GSK-3
HDAC
|
Neurological Disease
|
|
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/Histone Deacetylases (GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
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-
- HY-103018S
-
|
ASN-002-d4
|
Isotope-Labeled Compounds
JAK
Syk
|
Inflammation/Immunology
Cancer
|
|
Gusacitinib-d4 (ASN-002-d4) is the deuterium labeled Gusacitinib (HY-103018). Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-162367
-
|
|
FLT3
Checkpoint Kinase (Chk)
|
Cancer
|
|
FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-174302
-
|
|
Pim
HDAC
PARP
Apoptosis
|
Cancer
|
|
PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-146749
-
|
|
FLT3
Trk Receptor
Apoptosis
|
Cancer
|
|
FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .
|
-
- HY-177515
-
|
|
IRAK
STAT
JAK
NF-κB
|
Inflammation/Immunology
|
|
IRAK4 modulator-2 (Compound 5) is a selective dual Interleukin-1 Receptor Associated Kinase 4 (IRAK4) and IRAK1 inhibitor with IC50 values of 0.005 μM and 0.97 μM, erespectively. IRAK4 modulator-2 blocks IRAK-mediated signaling pathways (e.g., JAK-STAT, NF-κB pathways), reduces the production of pro-inflammatory cytokines (e.g., IL-1, TNF), and exerts anti-inflammatory activity. IRAK4 modulator-2 is promising for research of autoimmune diseases and inflammatory diseases, such as rheumatoid arthritis, psoriasis, inflammatory bowel disease .
|
-
- HY-178441
-
|
|
Pyruvate Kinase
Reactive Oxygen Species (ROS)
Apoptosis
Microtubule/Tubulin
|
Metabolic Disease
Cancer
|
|
PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer .
|
-
- HY-178029
-
|
|
Ribosomal S6 Kinase (RSK)
Topoisomerase
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
|
Cancer
|
|
RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-N0737AG
-
|
Telepathine (GMP)
|
Fluorescent Dye
|
|
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
|
| Cat. No. |
Product Name |
Type |
-
- HY-N0737AG
-
|
Telepathine (GMP)
|
Biochemical Assay Reagents
|
|
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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