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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC46945 Avotaciclib
Avotaciclib (BEY1107) is an orally active cyclin dependent kinase 1 (CDK1) inhibitor. Avotaciclib can be used for the research of cancer.
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DC46944 Ipivivint
Ipivivint (SM08502), a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer.
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DC46942 CCR4 antagonist 3 hydrochloride
CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.
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DC46941 Cl-4AS-1
Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively).
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DC46939 Thalidomide-O-PEG4-amine hydrochloride
Thalidomide-O-PEG4-amine hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
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DC46938 Thalidomide-O-PEG4-amine TFA
Thalidomide-O-PEG4-amine TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
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DC46937 Seco-DUBA
Seco-DUBA is a duocarmycin (DUBA) prodrug containing two hydroxyl groups, which can each be used for coupling to an antibody via a linker. Seco-DUBA can be used in the synthesis of antibody-drug conjugates (ADCs).
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DC46936 JW67
JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth.
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DC46935 SR-1277
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer.
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DC46934 (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM.
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DC46933 Timtraxanib
Timtraxanib (AVI-3207) is a selective VEGF-2 inhibitor. Timtraxanib can be used for the research of senile macular degeneration.
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DC46932 Luxeptinib
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.
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DC46931 Gunagratinib
Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer.
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DC46929 Erlotinib-13C6
Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR.
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DC46928 TL-895
TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively. TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research.
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DC46927 PF-03622905
PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases.
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DC46926 Bisindolylmaleimide XI hydrochloride
Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively.
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DC46923 SKF-86002 dihydrochloride
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
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DC46920 Dazcapistat
Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively (patent WO2018064119A1, compound 405).
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DC46919 AKT-IN-6
AKT-IN-6 (Example 13) is a potent Akt inhibitor. AKT-IN-6 inhibits Akt1, Akt2 and Akt3 with IC50s < 500nM, respectively. (patent WO2013056015A1).
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DC46918 Vevorisertib
Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations.
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DC46915 N-Desethyl Sunitinib hydrochloride
N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.
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DC46914 Q134R
Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer's disease (AD) and aging-related disorders research.
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DC46912 ABC-1
ABC-1 is a phosphorylated analogue and a potential antiviral agent against Newcastle disease virus (NDV). ABC-1 has potent antiviral activity.
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DC46911 SPOP-IN-6b hydrochloride
SPOP-IN-6b hydrochloride is a potent speckle-type POZ protein (SPOP) inhibitor with an IC50 of 3.58 μM.
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DC46909 (-)-Chromanol 293B
(-)-Chromanol 293B is a potent and selective inhibitor of the slow component of delayed rectifier K+ current (IKs). (-)-Chromanol 293B can be used for the research of antiarrhythmic.
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DC46908 PSB069
PSB069 bearing a p-chlorophenylamino residue is a potent, well-tolerated and nonselective NTPDases1, 2, 3 inhibitor(Ki=16~18 μM).
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DC46907 AM-8123
AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.
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DC46906 Odatroltide
Odatroltide, as a nanoscale P-selectin inhibitor, is a nano-delivery system of 6,7-dihydroxyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and KPAK to target the thrombus.
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DC46905 Seletracetam lithium bromide
Seletracetam (Ucb 44212) lithium bromide, an analog of the antiepileptic agent Levetiracetam, is a SV2A modulator for the research of epilepsy.
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