Search Result
Results for "
multiple kinase inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Bibliotecas de Screening
5
Isotope-Labeled Compounds
| Cat. No. |
Nombre del producto |
Target |
Áreas de investigación |
Chemical Structure |
-
- HY-14596
-
Genistein
Maximum Cited Publications
88 Publications Verification
NPI 031L
|
EGFR
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
|
-
-
- HY-12137
-
|
BI 6727
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
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Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
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-
-
- HY-148810
-
|
BI 1810631
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c-Met/HGFR
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Cancer
|
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Zongertinib (BI 1810631) is a potent and selective HER2 and EGFR tyrosine kinase inhibitor with IC50 values of 13 nM and 579 nM, respectively. Zongertinib has antitumor activity and can be used in the study of multiple solid tumors .
|
-
-
- HY-112306
-
|
DCC-2618
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
|
Cancer
|
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Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
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-
-
- HY-12044
-
|
XL184 S-malate; BMS-907351 S-malate
|
VEGFR
Apoptosis
|
Cancer
|
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Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
-
- HY-138696
-
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XL092
|
TAM Receptor
c-Met/HGFR
VEGFR
|
Cancer
|
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Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research .
|
-
-
- HY-15160
-
TAK-960
2 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
-
- 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-15728
-
|
IY-5511
|
Bcr-Abl
Apoptosis
STAT
JAK
Prion Protein
|
Infection
Neurological Disease
Cancer
|
|
Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases .
|
-
-
- HY-N0031
-
-
-
- HY-118266
-
BTdCPU
3 Publications Verification
|
Phosphatase
Apoptosis
|
Cancer
|
|
BTdCPU is a potent heme regulated inhibitor kinase (HRI) activator that promotes eIF2α phosphorylation and induces apoptosis in Dexamethasone (HY-14648) (Dex)-resistant cancer cells. BTdCPU can be used in the study of cancers such as multiple myeloma and Dex-resistant multiple myeloma .
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-
-
- HY-B1165
-
|
|
p38 MAPK
Checkpoint Kinase (Chk)
Histamine Receptor
5-HT Receptor
CDK
PARP
Apoptosis
|
Cancer
|
|
Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .
|
-
-
- HY-14596S
-
|
NPI 031L-d4
|
EGFR
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Genistein-d4 is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis .
|
-
-
- HY-13016S
-
|
XL184-d6; BMS-907351-d6
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively .
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-
-
- HY-150617
-
|
M4076; ATM inhibitor-5
|
ATM/ATR
STING
PD-1/PD-L1
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
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-
-
- HY-123981
-
5MPN
3 Publications Verification
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
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- HY-14596R
-
|
NPI 031L (Standard)
|
Reference Standards
EGFR
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Genistein (Standard) is the analytical standard of Genistein. This product is intended for research and analytical applications. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
|
-
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- HY-16976
-
|
|
Pim
|
Cancer
|
|
GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma .
|
-
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- HY-109192
-
|
SAR442168; PRN2246
|
Btk
|
Neurological Disease
|
|
Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS) .
|
-
-
- HY-109082
-
|
SKI-O-703
|
Syk
|
Inflammation/Immunology
|
|
Cevidoplenib (SKI-O-703) is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities. Cevidoplenib is also the mesylate form of SKI-O-592. Cevidoplenib and SKI-O-592 inhibits BCR-mediated survival, proliferation, and differentiation of B cells. And SKI-O-592 potently inhibits multiple kinases with IC50s of 6.2 nM (Syk), 1.859 μM (Jak2), 5.807 μM (Jak3), 0.412 μM (RET), 0.687 μM (KOR), 1.783 μM (FLT3), 16.96 μM (FGFR1), 5.662 μM (FGFR3), and 0.709 μM (Pyk2), respectively .
|
-
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- HY-N0442
-
-
-
- HY-142817
-
|
|
G Protein-coupled Receptor Kinase (GRK)
Aurora Kinase
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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 .
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-
-
- HY-141687
-
|
|
CDK
Apoptosis
|
Cancer
|
|
NSC 107512 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9). NSC 107512 is a class of sangivamycin-like molecules (SLM). NSC 107512 inhibits growth and induces apoptosis of multiple myeloma tumors .
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-
-
- HY-12137A
-
|
BI 6727 trihydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
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-
-
- HY-112411
-
|
|
EGFR
ERK
PDGFR
FGFR
|
Neurological Disease
Inflammation/Immunology
|
|
PD 174265 is a highly selective, reversible EGFR/ErbB2 tyrosine kinase inhibitor (IC50=0.45 nM) and cell differentiation inducer. By blocking receptor autophosphorylation and the downstream ERK signaling pathway (with an IC50 of 0.45 μM for full-length ERK), PD 174265 effectively inhibits tumor growth and exhibits antitumor activity without obvious toxicity in in vivo models. PD 174265 drives oligodendrocyte precursor cells to switch from a proliferative state to a differentiated state, significantly upregulates the expression of myelin proteins such as CNP, PLP and MBP, and induces neurite branching. PD 174265 shows no inhibitory effect on other kinases including insulin, PDGF and basic FGF receptors, and serves as a crucial tool molecule for investigating the treatment of human epidermoid carcinoma and the mechanism of myelin repair in multiple sclerosis .
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-
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- HY-126328
-
|
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PKC
Interleukin Related
|
Inflammation/Immunology
|
|
PKC-theta inhibitor 1 is an orally active and selective ATP-competitive inhibitor of Protein Kinase Cθ (PKCθ), with a Ki value of 6 nM. PKC-theta inhibitor 1 inhibits T-cell-mediated inflammatory responses by suppressing the release of proinflammatory cytokines (IL-2 IC50 = 0.21 μM in anti-CD3/CD28-stimulated PBMCs; IL-17 IC50 = 1 μM in CD3/CD28-stimulated Th17 cells) PKC-theta inhibitor 1 significantly reduces symptoms in mice with ongoing experimental autoimmune encephalomyelitis (EAE). PKC-theta inhibitor 1 can be used for the study of T-cell-mediated inflammatory diseases such as multiple sclerosis .
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-
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- HY-164795
-
|
|
Neurotensin Receptor
Arrestin
iGluR
ERK
Sodium Channel
|
Neurological Disease
|
|
SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .
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-
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- HY-164795A
-
|
|
Neurotensin Receptor
Arrestin
iGluR
ERK
Sodium Channel
|
Neurological Disease
|
|
SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .
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-
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- HY-P5904
-
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Caveolin-1 scaffolding domain peptide
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c-Met/HGFR
|
Others
|
|
Caveolin-1 (82-101) amide (human, mouse, rat) (Caveolin-1 scaffolding domain peptide) is a peptide that reverses aging-associated deleterious changes in multiple organs. Caveolin-1 (82-101) amide (human, mouse, rat) inhibits tyrosine kinases .
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-
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- HY-163565
-
|
|
Btk
|
Neurological Disease
|
|
BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. BIIB129 can be used in multiple sclerosis (MS) research .
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-
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- HY-16462
-
|
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CDK
|
Cancer
|
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CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.
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-
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- HY-153077
-
-
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- HY-16129
-
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Calmodulin
Checkpoint Kinase (Chk)
MAPKAPK2 (MK2)
MAP3K
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Cancer
|
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CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser 216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer .
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-
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- HY-117102
-
|
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Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
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Cancer
|
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
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-
-
- HY-117548
-
UNC1062
2 Publications Verification
|
TAM Receptor
Apoptosis
p38 MAPK
ERK
PI3K
Akt
JAK
STAT
|
Cardiovascular Disease
Cancer
|
|
UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis .
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-
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- HY-13016S1
-
|
XL184-d4; BMS-907351-d4
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
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-
-
- HY-128879
-
|
|
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-175525
-
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PROTACs
Aurora Kinase
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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)) .
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-
-
- HY-149636
-
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EGFR
CDK
VEGFR
Apoptosis
|
Cancer
|
|
Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells .
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-
-
- HY-163471
-
|
|
PDGFR
VEGFR
|
Cancer
|
|
PDGFRα/β/VEGFR-2-IN-1 (6f), a multiple PDGFRα/ and VEGFR-2 tyrosine kinase inhibitor, particularly targets PDGFRα, PDGFRβ, and VEGFR-2 kinases with Nano molar concentrations .
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-
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- HY-12470A
-
|
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Casein Kinase
|
Cancer
|
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PF-4800567 hydrochloride is a potent and selective inhibitor of?casein kinase?1? (CK1?), with an?IC50?of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 hydrochloride is useful in probing unique roles between these two kinases in multiple signaling pathways .
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-
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- HY-15160B
-
|
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Polo-like Kinase (PLK)
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Cancer
|
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
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-
-
- HY-15160A
-
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Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
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-
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- 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 .
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-
-
- HY-178133
-
|
|
Pim
Apoptosis
Caspase
|
Cancer
|
|
Pim-1 kinase-IN-14 is a PIM-1 kinase inhibitor with an IC50 value of 94 nM. Pim-1 kinase-IN-14 shows broad-spectrum and high-efficiency anticancer activity against multiple human cancer cell lines, including liver cancer (HepG-2), colon cancer (Caco-2), myeloid leukemia (NFS-60), and prostate cancer (PC-3) cells. Pim-1 kinase-IN-14exerts its anticancer effects by inducing apoptosis and activating caspase 3/7. Pim-1 kinase-IN-14 can be used for the study of cancers associated with PIM-1 kinase overexpression .
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-
-
- HY-174256
-
-
-
- HY-157871
-
|
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MAP3K
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Cancer
|
|
TAK1-IN-5 (Compound 26) is an inhibitor of the transforming growth factor-β activated kinase (TAK1) with an IC50 value of 55 nM. TAK1-IN-5 can inhibit the growth of MPC-11 and H929 cells with a GI50 lower than 30 nM. TAK1-IN-5 can be used in the study of multiple myeloma .
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-
-
- HY-150617A
-
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(Rac)-M4076; (Rac)-ATM inhibitor-5
|
ATM/ATR
STING
PD-1/PD-L1
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
(Rac)-Lartesertib ((Rac)-M4076) is an isoform of Lartesertib (HY-150617). Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
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-
-
- HY-107592
-
|
|
IKK
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
|
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ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies .
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-
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- HY-12137R
-
|
BI 6727 (Standard)
|
Polo-like Kinase (PLK)
Apoptosis
Reference Standards
|
Cancer
|
|
Volasertib (Standard) is the analytical standard of Volasertib. This product is intended for research and analytical applications. Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
|
-
- HY-112306R
-
|
DCC-2618 (Standard)
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
Reference Standards
|
Cancer
|
|
Ripretinib (Standard) is the analytical standard of Ripretinib. This product is intended for research and analytical applications. Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
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- HY-16129A
-
|
|
Calmodulin
MAP3K
MAPKAPK2 (MK2)
Checkpoint Kinase (Chk)
|
Cancer
|
|
CBP-501 acetate, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser 216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 acetate is used for various types of cancer .
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-
- 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-149019
-
|
|
c-Kit
Apoptosis
|
Cancer
|
|
Antitumor agent-70 (compound 8b) has anti-tumor activity and can induce cell apoptosis. Antitumor agent-70 inhibits multiple myeloma with an IC50 value of 0.12 μM. Antitumor agent-70 is a potential multi-targeted kinase inhibitor especially for c-Kit .
|
-
- HY-155804
-
|
|
Necroptosis
RIP kinase
|
Inflammation/Immunology
|
|
RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species .
|
-
- HY-178344
-
|
|
Calcium Channel
Sodium Channel
|
Cardiovascular Disease
|
|
Multi-target kinase-IN-6 is a Multiple target kinase inhibitor. Multi-target kinase-IN-6 can inhibit cardiac RyR2- and NaV1.5-channels but stimulate SERCA2a pump activity. Multi-target kinase-IN-6 can be used for the research of cardiovascular disease, such as heart failure .
|
-
- HY-120744
-
|
|
Tau Protein
|
Others
|
|
LDN-193665 is a Tau kinase inhibitor with tauopathy-modifying activity. LDN-193665 inhibits Tau phosphorylation, improves tauopathy in animal models, reduces Sarkosyl-insoluble Tau, and restores memory. It may be necessary to simultaneously target multiple kinases to effectively inhibit tauopathies.
|
-
- 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-164413
-
|
|
VEGFR
EGFR
RET
Apoptosis
|
Cancer
|
|
CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
|
-
- HY-121708
-
|
|
c-Kit
|
Cancer
|
|
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
|
-
- HY-15160C
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-163267
-
|
|
Fluorescent Dye
|
Others
|
|
ZNL0325 is a covalent probe based on pyrazolopyrimidine. ZNL0325 features an acrylamide side chain at the C3 position, which is capable of forming covalent bonds with multiple kinases that possess a cysteine at the αD-1 position, including BTK, EGFR, BLK, and JAK3. ZNL0325 can be used in the research of creating structurally distinct covalent kinase inhibitors .
|
-
- HY-159996
-
-
- HY-17651
-
|
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
PI3K-IN-60 (Compound 34) is a highly selective phosphatidylinositol 3-kinase gamma (PI3Kγ) inhibitor. PI3K-IN-60 is promising for research of autoimmune diseases (e.g., multiple sclerosis) and cancers (e.g., breast cancer, pancreatic ductal adenocarcinoma) .
|
-
- HY-13590
-
|
|
VEGFR
|
Cancer
|
|
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
|
-
- HY-147864
-
|
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis .
|
-
- HY-135216
-
|
|
Src
VEGFR
Raf
EGFR
|
Cancer
|
|
Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC50 of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC50 of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-110333
-
|
|
EGFR
|
Cancer
|
|
BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .
|
-
- HY-12044R
-
|
XL184 S-malate (Standard); BMS-907351 S-malate (Standard)
|
Reference Standards
VEGFR
Apoptosis
|
Cancer
|
|
Cabozantinib (S-malate) (Standard) is the analytical standard of Cabozantinib (S-malate). This product is intended for research and analytical applications. Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
- HY-100833R
-
|
|
Reference Standards
Bacterial
Antibiotic
|
Infection
|
|
Cabozantinib (S-malate) (Standard) is the analytical standard of Cabozantinib (S-malate). This product is intended for research and analytical applications. Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
- HY-19471
-
|
|
Drug Isomer
CDK
VEGFR
Survivin
Apoptosis
|
Cancer
|
|
(rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET .
|
-
- HY-149718
-
|
|
JAK
HDAC
|
Cancer
|
|
Antitumor agent-123 (Copmound 4d) effectively inhibits multiple kinase targets with anti-cancer effects, including JAK2, JAK3, HDAC1 and HDAC6, with IC50 values of 34.6 and 2.6 μM for JAK2 and JAK3, respectively. Antitumor agent-123 exhibits moderate activity in solid tumor models .
|
-
- 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-136841
-
|
|
CDK
|
Cancer
|
|
SLM6 is a sangivamycin-like molecule. SLM6 is a CDK9 inhibitor. SLM6 inhibits CDK9/cyclin K and CDK9/cyclin T1 kinase activity with IC50s of 280 nM and 133 nM, respectively. SLM6 also inhibits CDK1/cyclin B and CDK2/
cyclin A with IC50s of less than 300 nM. SLM6 induces apoptosis in multiple myeloma (MM) cells .
|
-
- HY-15728S
-
|
IY-5511-d6
|
Isotope-Labeled Compounds
Bcr-Abl
Apoptosis
STAT
JAK
Prion Protein
|
Infection
Neurological Disease
Cancer
|
|
Radotinib-d6 is deuterium labeled Radotinib (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases .
|
-
- HY-W706452
-
|
XL184-d4 S-malate; BMS-907351-d4 S-malate
|
Isotope-Labeled Compounds
Apoptosis
VEGFR
|
Cancer
|
|
Cabozantinib-d4 (S-malate) (XL184-d4 (S-malate); BMS-907351-d4 (S-malate)) is the deuterium labeled Cabozantinib (S-malate) (HY-12044). Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
- HY-151154
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .
|
-
- HY-123237
-
|
|
c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
|
-
- HY-N0031R
-
|
|
Reference Standards
NF-κB
PI3K
Apoptosis
Autophagy
p38 MAPK
Src
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Plantamajoside (Standard) is the analytical standard of Plantamajoside. This product is intended for use in research and analytical applications. Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects .
|
-
- HY-N0442R
-
|
4'-O-β-D-Glucosyl-5-O-methylvisamminol (Standard)
|
Reference Standards
p38 MAPK
Reactive Oxygen Species (ROS)
TNF Receptor
MEK
ERK
VEGFR
Src
Amyloid-β
Anaplastic lymphoma kinase (ALK)
NF-κB
NOD-like Receptor (NLR)
JNK
Ferroptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) (Standard) is the analytical standard of 5-O-Methylvisammioside. This product is intended for research and analytical applications. 5-O-Methylvisammioside is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.
|
-
- HY-117222
-
|
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
AM-0216 is a highly selective NF-κB-inducing kinase (NIK) inhibitor with a Ki value of 2 nM. AM-0216 is promising for research of NF-κB-dependent hematologic malignancies (e.g., multiple myeloma) and autoimmune diseases .
|
-
- HY-124865
-
|
|
MAP3K
IKK
|
Cancer
|
|
MAP3K14-IN-1 (Compound 173) is a MAP3K14 (NIK kinase) inhibitor with an IC50 of 1.8 nM. MAP3K14-IN-1 inhibits the autophosphorylation of MAP3K14 kinase. MAP3K14-IN-1 reduces the level of phosphorylated IKKα in cancer cells. MAP3K14-IN-1 inhibits the proliferation of multiple myeloma cells. MAP3K14-IN-1 can be used in research related to multiple myeloma .
|
-
- HY-181586
-
|
|
Casein Kinase
|
Others
|
CK1γ-IN-1 is a non-selective CK1 kinase inhibitor with IC50 values of 780 nM, 570 nM and 990 nM against human CK1γ1, CK1γ2, CK1γ3, respectively. The non-specific binding of CK1γ-IN-1 to multiple kinases enables its application in biological studies of specific CK1γ .
|
-
- HY-N17632
-
|
|
Estrogen Receptor/ERR
Akt
MELK
COX
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Moracin G is a plant-derived kinase modulator and receptor ligand that forms stable bindings with multiple key proteins (AKT1, COX2 and Estrogen receptor 1) and competitively inhibits the activity of specific kinases. By binding to MELK to disrupt cell cycle regulation, Moracin G impairs the survival and proliferation of cancer cells, induces cancer cell apoptosis, and thereby exerts anti-tumor potential. Moracin G can be used in research related to periodontitis and breast cancer .
|
-
- HY-182037
-
|
|
DNA/RNA Synthesis
Pyruvate Kinase
|
Cancer
|
|
Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research .
|
-
- HY-179460
-
|
IY-5511 dihydrochloride
|
Bcr-Abl
Apoptosis
STAT
JAK
Prion Protein
|
Neurological Disease
Cancer
|
|
Radotinib (IY-5511) dihydrochloride is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib dihydrochloride has anti-prion and anti-tumor activities. Radotinib dihydrochloride can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib dihydrochloride can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases .
|
-
- HY-181166
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-194 is a potent EGFR tyrosine kinase inhibitor with an IC50 of 54.3 nM against human EGFR. EGFR-IN-194 induces apoptosis, inhibits migration in cancer cells, selectively promotes invasion in cancer cells, and exhibits antiproliferative effects across multiple cancer cell lines. EGFR-IN-194 can be used for the research of prostate adenocarcinoma, non-small cell lung carcinoma, breast carcinoma, chronic myeloid leukemia .
|
-
- HY-181585
-
|
|
Casein Kinase
|
Others
|
|
FP1-24 is a non-selective CK1 kinase inhibitor, with IC50 values of 40 nM, 10 nM, 10 nM, and 40 nM against human CK1γ1, CK1γ2, CK1γ3 and CK1δ, respectively. FP1-24 exerts its activity by reducing the phosphorylation level of LRP5/6 at the T1479 site during WNT signaling pathway activation. The non-specific binding of FP1-24 to multiple kinases can be used for biological studies of specific CK1γ .
|
-
- HY-18746
-
|
|
Parasite
PI4K
|
Infection
|
|
KAI-407 is an orally active inhibitor of Plasmodium PI4K kinase, which can broadly inhibit multiple stages of the parasite lifecycle. KAI-407 exhibits EC50s of for the blood stage of malignant Plasmodium of 81 nM; for the liver schizonts of P. yoelii of 88 nM; and IC50s for the liver schizonts and dormant bodies of P. cynomolgi of 0.64 μM and 0.69 μM respectively. KAI-407 can prevent Plasmodium berghei infection 100%. KAI-407 can be used for the study of vivax malaria .
|
-
- HY-115541
-
|
|
Epigenetic Reader Domain
JAK
FLT3
RET
ROS Kinase
PDGFR
FGFR
c-Myc
STAT
Apoptosis
PARP
|
Cancer
|
|
BRD4-IN-41 is a BRD4 inhibitor with an IC50 of 34 nM. BRD4-IN-41 also inhibits JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC50 values ranging from 0.9 nM to 43 nM. BRD4-IN-41 inhibits acetyl-lysine binding site of BRD4, downregulates c-MYC, reduces phosphorylated STAT3 levels, induces G1 cell cycle arrest and apoptosis, thereby inhibiting cancer cells growth. BRD4-IN-41 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia .
|
-
- HY-20888
-
|
MNF
|
Aryl Hydrocarbon Receptor
Cytochrome P450
Apoptosis
Akt
ERK
TGF-beta/Smad
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
3'-Methoxy-4'-nitroflavone (MNF) is a specific aryl hydrocarbon receptor (AhR) antagonist. 3'-Methoxy-4'-nitroflavone activates AhR by inhibiting CYP1, the metabolic enzyme of the endogenous ligand FICZ (HY-12451), leading to the accumulation of FICZ. 3'-Methoxy-4'-nitroflavone reverses the anti-apoptotic effect of TCDD, attenuates the activation of Akt and Erk1/2 kinases and the expression of TGFα induced by TCDD. 3'-Methoxy-4'-nitroflavone can be used in research related to breast tumor promotion, rheumatoid arthritis, multiple sclerosis and inflammatory bowel disease .
|
-
| Cat. No. |
Nombre del producto |
|
-
-
HY-L158
-
|
|
6,135 compounds
|
|
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 6,135 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes
|
| Cat. No. |
Nombre del producto |
Target |
Research Area |
-
- HY-P5904
-
|
Caveolin-1 scaffolding domain peptide
|
c-Met/HGFR
|
Others
|
|
Caveolin-1 (82-101) amide (human, mouse, rat) (Caveolin-1 scaffolding domain peptide) is a peptide that reverses aging-associated deleterious changes in multiple organs. Caveolin-1 (82-101) amide (human, mouse, rat) inhibits tyrosine kinases .
|
-
- HY-16129
-
|
|
Calmodulin
Checkpoint Kinase (Chk)
MAPKAPK2 (MK2)
MAP3K
|
Cancer
|
|
CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser 216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer .
|
-
- HY-16129A
-
|
|
Calmodulin
MAP3K
MAPKAPK2 (MK2)
Checkpoint Kinase (Chk)
|
Cancer
|
|
CBP-501 acetate, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser 216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 acetate is used for various types of cancer .
|
| Cat. No. |
Nombre del producto |
Category |
Target |
Chemical Structure |
| Cat. No. |
Nombre del producto |
Chemical Structure |
-
- HY-14596S
-
|
|
|
Genistein-d4 is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis .
|
-
-
- HY-13016S
-
|
|
|
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively .
|
-
-
- HY-13016S1
-
|
|
|
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
-
- HY-15728S
-
|
|
|
Radotinib-d6 is deuterium labeled Radotinib (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases .
|
-
-
- HY-W706452
-
|
|
|
Cabozantinib-d4 (S-malate) (XL184-d4 (S-malate); BMS-907351-d4 (S-malate)) is the deuterium labeled Cabozantinib (S-malate) (HY-12044). Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
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