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RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .
A 83-01 is a potent inhibitor of TGF-β typeI receptor ALK5 kinase, typeI nodal receptor ALK4 and typeI nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively .
VI 16832 is a broad spectrum TypeIkinase inhibitor which can be used as an enrichment tool for the comparative expression analysis of protein kinases in different cancer cell lines.
LY2857785 is a typeI reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinasesCDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315Ikinase protein, respectively .
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of typeI DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol .
GEM231 sodium is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinasetypeI ). GEM231 sodium induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
GEM231 is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinasetypeI ). GEM231 induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
PPY-A is a potent T315I mutant and wild-typeAblkinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba⁄F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML) .
TGFβRI-IN-1 is an oral active and selective TGFβ receptor typeI (TGFβRI)kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
A 83-01 sodium is a potent inhibitor of TGF-β typeI receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively .
ALK5-IN-10 (Compound 5d) is a TGF-β typeI receptor kinaseALK5 inhibitor, with IC50s of 0.007 and 1.98 μM for ALK5 and p38α, respectively. ALK5-IN-10 can be used for the research of cancer .
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK typeI family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes .
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
IN-1130 is a highly selective transforming growth factor-β typeI receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible typeI inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells .
Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible typeI inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells .
LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) [2]
The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the TypeI receptor. The typeI receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc.
MCE designs a unique collection of 226 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.
CAMK1 Protein, Human (HEK293, His), a recombinant human CAMK1 produced in HEK293 cells, has a His tag at the N-terminus. CAMK1 is involved in multiple cell functions, including calmodulin binding, ATP binding, signal transduction, development and cell differentiation.
The PNCK protein is a calcium/calmodulin-dependent protein kinase and a key component of the calcium-triggered signaling cascade. In vitro, PNCK exhibits the ability to phosphorylate CREB1 and SYN1/synapsin I, emphasizing its involvement in regulating cellular processes associated with these substrates. PNCK Protein, Human (Sf9, GST) is the recombinant human-derived PNCK protein, expressed by Sf9 insect cells , with GST tagged. The total length of PNCK Protein, Human (Sf9, GST) is 342 a.a., .
The PNCK protein is a calcium/calmodulin-dependent protein kinase and a key component of the calcium-triggered signaling cascade. In vitro, PNCK exhibits the ability to phosphorylate CREB1 and SYN1/synapsin I, emphasizing its involvement in regulating cellular processes associated with these substrates. PNCK Protein, Human (Sf9, His, GST) is the recombinant human-derived PNCK protein, expressed by Sf9 insect cells , with N-8*His, N-GST labeled tag. The total length of PNCK Protein, Human (Sf9, His, GST) is 342 a.a., .
PRKAR1A protein is a regulatory subunit of cAMP-dependent protein kinase that mediates cellular responses to cAMP signaling. The inactive holoenzyme has two regulatory chains and two catalytic chains. PRKAR1A Protein, Mouse (sf9, His) is the recombinant mouse-derived PRKAR1A protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of PRKAR1A Protein, Mouse (sf9, His) is 381 a.a., with molecular weight of ~44.6 kDa.
