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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC77205 WAY-606344
WAY-606344 (Compound 97) is a Casein kinase 1δ inhibitor. WAY-606344 is promising for research of Alzheimer's disease.
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DC77204 CK1δ/CK1ε liagnd-1
CK1δ/CK1ε liagnd-1 is the ligand for CK1δ/CK1ε that can be used for synthesis of CK1 PROTAC degrader AH078.
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DC77203 AH078
AH078 (compound 37) is a PROTAC degrader that selectively targets CK1δ and CK1ε, and has low targeting for CK1α.
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DC77202 (R,R)-BMS-986397
(R,R)-BMS-986397 is a CK1α degrader (DC50 between 0.1-0.5 pM). (R,R)-BMS-986397 can be used in anti-leukemia research.
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DC77201 Lenvatinib N-oxide
Lenvatinib N-Oxide (Lenvatinib impurity 10) is the impurity of Lenvatinib. DCG04 is a multivalent ligand for the mannose-6-phosphate receptor. DCG-04 is an activity-based probe for cysteine cathepsins, and can be used for labelling numerous cysteine cathepsins in cell and tissue lysates.
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DC77200 (Z)-SU14813
(Z)-SU14813 is an analog of SU14813. CAY10568 is physically smaller and less hydrophobic than the QX-314. CAY10568 can be used in studies of inflammation and pain perception.
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DC77199 VMD-928
VMD-928 is an orally active, allosteric, irreversible and selective tropomyosin receptor kinase A (TrkA) inhibitor. VMD-928 blocks the downstream signaling pathways triggered by the binding of nerve growth factor (NGF) to TrkA, thereby inhibiting cell proliferation, invasion, and promoting cancer cell death. VMD-928 is promising for research of various cancers, including prostate cancer, thymic carcinoma, mesothelioma, squamous cell carcinoma of the head and neck, squamous cell carcinoma of the lung, ovarian cancer, hepatocellular carcinoma.
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DC77198 BNN27
BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable.
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DC77197 TG-100435
TG-100435 is a multitargeted, orally active protein tyrosine kinase inhibitor, with Ki of 13 to 64 nM for Src, Lyn, Abl, Yes, Lck, and EphB4. TG-100435 plays an important role in cancer research.
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DC77196 RK-20448
RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC50 values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259 derivative with neuroprotective and PP2A activating activities. FTY720-Mitoxy has the property of targeting mitochondria. In addition, FTY720-Mitoxy protects neurons by reducing inflammatory responses and is used in the study of neurodegenerative diseases such as Parkinson's disease.
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DC77195 K882
K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer.
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DC77194 CGP062464
CGP062464 is an inhibitor of the tyrosine kinase c-Src (IC50: < 50 nM). CGP062464 can be used for research of osteoporosis and tumor-induced hypercalcemia.
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DC77193 Xanthinol
Xanthinol is a potent modulator of tumor hemodynamics.
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DC77192 RPR-101511
RPR-101511 is a 3-substituted quinoline derivative. RPR-101511 is a PDGF receptor tyrosine kinase inhibitor (IC50: 0.001-0.02 μM).
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DC77191 2-Methyl-3-phenylquinoxaline
2-Methyl-3-phenylquinoxaline (compound 38) is a potent platelet-derived growth factor receptor tyrosine kinase (PDGF-RTK) inhibitor with modest inhibitory activity against PDGFR kinase in intact cells (IC50 greater than 100 μM).
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DC77190 DDN
DDN is a selective insulin receptor (Insulin Receptor) activator, an insulin sensitizer, and a glucose-lowering insulin mimetic with oral bioavailability. DDN can directly bind to the receptor kinase domain and induce Akt and ERK phosphorylation, and it can also enhance insulin's effect on glucose uptake. DDN significantly reduces blood glucose levels in wild-type and diabetic ob/ob and db/db mice.
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DC77189 Lomonitinib
Lomonitinib is a highly potent and selective pan-FLT3/IRAK4 inhibitor with antitumor activity. Lomonitinib is promising for research of myeloid leukemia.
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DC77188 HSN748
HSN748 is a Ponatinib, and exhibits inhibitory activity against heparanase. Pixatimod free acid binds to the S1 receptor binding domain (RBD) of the SARS-CoV-2 virus, that inhibits SARS-CoV-2 isolate strains with EC50 of 2.4-13.8 µg/mL. Pixatimod free acid is an agonist for TLR9 signaling pathway, enhances the activity of dendritic cells (DCs), activates natural killer cells, and exhibits immunomodulatory and anti-tumor activities.
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DC77187 FW-1
FW-1 is a type I inhibitor for FLT3 with IC50 of ca. 1 μM. FW-1 exhibits cytotoxicity in FLT3 mutated AML cell. FW-1 arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell MV4-11 and MOLM-13.
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DC77186 Clifutinib
Clifutinib (Compound 9e) is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.
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DC77185 CHEMBL4444839
CHEMBL4444839 is an inhibitor of FLT3 and can be used in the research of acute myeloid leukemia (AML).
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DC77184 CG-3-246
CG-3-246 is a dual inhibitor of FLT3/BCL-2, with the Kds of 63 and 4.25 nM, respectibely. CG-3-246 plays an important role in acute myeloid leukemias research.
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DC77183 Siphonaxanthin
Siphonaxanthin is a keto-carotenoid with anti-angiogenic and anti-inflammatory activity, which is found in green algae. Siphonaxanthin upregulates the expression of death receptor 5 (DR5), induces cancer cell apoptosis, decreases the expression of Bcl-2, and activates caspase-3. Siphonaxanthin is also an inhibitor of FGFR-1. Siphonaxanthin inhibits the proliferation, migration, and tube formation of human umbilical vein endothelial cells (HUVECs), as well as the outgrowth of microvessels in the rat aortic ring. Siphonaxanthin is promising for research of diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.
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DC77182 PNU-145156E
PNU-145156E (FCE26644) is an angiogenesis inhibitor with anti-tumor activity. PNU-145156E inhibits the binding of bFGF to its receptor and inhibits bFGF-induced endothelial cell proliferation and motility.
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DC77181 BW710
BW710 is an orally active fibroblast growth factor receptor 2 (FGFR2) inhibitor. BW710 inhibits the proliferation of BaF3-FGFR2 cells with an IC50 of 2.8 nM. BW710 abolishes FGFR2 enzymatic activity and is selective against other 75 tyrosine kinases including FGFR1, FGFR3, and FGFR4 at 1 μM. BW710 suppresses the FGFR2 signaling and selectively inhibits FGFR2-driven cancer cell proliferation. BW710 displays reasonable pharmacokinetic properties with an oral bioavailability of 29 % in mice.
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DC77180 Befotertinib mesylate
Befotertinib mesylate (D-0316 mesylate) is third-generation tyrosine kinase inhibitor (TKI) of EGFR . It can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
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DC77179 Asandeutertinib
Asandeutertinib (Osimertinib-d3, AZD-9291-d3) is an orally administered, ATP-competitive, irreversible, deuterated third-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor (EGFR TKI) and a deuterium-stabilized derivative of osimertinib, with the potential to treat advanced EGFR-mutated NSCLC.
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DC77178 ZJY-54
ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity.
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DC77177 TZEP7
TZEP7 is an EGFR kinase inhibitior in cancer cells. TZEP7 exhibits cytotoxic effects against cancer cell lines and induces apoptosis. TZEP7 demonstrates downregulation of antiapoptotic Bcl-2, upregulation of pro-apoptotic Bax, and increases caspase levels. TZEP7 is promising for research of anticancer agent.
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DC77176 Tyrphostin 63
Tyrphostin 63 (compound 13) is an epidermal growth factor receptor (EGFR) inhibitor with IC50 and Ki values are 375 and 123 μM, respectively.
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