atp-competitive

Pexidartinib (PLX-3397) is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

BI-D1870 is a cell-permeable, ATP-competitive inhibitor of ribosomal S6 kinases (RSKs; IC50s: 31/24/18/15 nM for RSK1/2/3/4).

LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure. LP-935509 is also an effective inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is a selective, ATP-competit

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Y-27632 (Y-27632) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Uprosertib (GSK2141795) (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.

GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.

Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Derazantinib (ARQ-087) (ARQ-087) is an ATP competitive tyrosine kinase inhibitor. It exhibits potent activity against FGFR1/FGFR2/FGFR3 chondrocytes (IC50s: 4.5 nM/1.8 nM/4.5 nM).

Gilteritinib (ASP2215) is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preClinicalal studies, gilteritinib showed strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 Clinicalal trials for acute myeloid leukemia.

GSK-3 Inhibitor XIII, an ATP-competitive GSK-3 inhibitor (Ki: 24 nM), can be used to study diabetes and obesity.

M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.

CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.

NU2058 (O(6)-Cyclohexylmethylguanine) is a guanine-based CDK inhibitor, also inhibits DNA topoisomerase II ATPase activity.

SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8/CycC, CDK19/CycC and CDK9/cycT. SEL120-34A possesses antitumor activity.

PF-3758309 hydrochloride (PF-03758309 hydrochloride) , is a PAK4 inhibitor, is also a n orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PF-3758309 hydrochloride binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.

AZD8931 is a reversible and ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 (IC50 of 4 nM, 3 nM and 4 nM, respectively).

A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16/46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th

PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

Capmatinib 2HCl (INC-280 2HCl) is a novel, ATP-competitive inhibitor of c-MET kinase with an IC50 with 0.13 nM.Capmatinib 2HCl exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10, 000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, Capmatinib 2HCl potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro.

SP-146 is a selective, potent and non-ATP-competitive Aurora B inhibitor(IC50 : 0.316 nM).

BAY 61-3606 (Syk inhibitor IV) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM), exhibiting no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.

N-Desethylsunitinib hydrochloride is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.

CK2α-IN-1 is a selective non-ATP-competitive CK2α inhibitor with an IC50 of 7.0 µM and a Ki of 1.6 µM.CK2α-IN-1 exhibits potential anticancer activity and can be used in cancer research.

IC 86621 is a selective and reversible ATP-competitive inhibitor of DNA-PK with an IC50 of 120 nM. IC 86621 increases DNA double-strand break(DSB)-induced antitumor activity with an EC50 of 68 µM for DNA-PK mediated cellular DSB repair.

SU9516 is a selectively potent ATP-competitive inhibitor of CDKs.

UNC 569 hydrochloride is a reversible and ATP-competitive inhibitor of Mer with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC 569 hydrochloride inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC 569 hydrochloride can be used in studies about acute lymphoblastic leukemia and atypical teratoid/rhabdoid tumors.

Capmatinib xHCl (INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor, potently blocking in vitro kinase activity (IC50 = 0.13 nM) as well as constitutive or HGF-stimulated activity in cells (IC50 values range from 0.3 to 1.1 nM).

PKG inhibitor peptide TFA (82801-73-8 free base) is an inhibitor of ATP-competitive cGMP-dependent protein kinase (PKG).

SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8/CycC and CDK19/CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor activity.

SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].

WYE-125132 (WYE-132 (WYE-125132)) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

ATR inhibitor 2 is an orally active, ATP-competitive, and selective ATR inhibitor (Ki <150 pM) with antitumor activity. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation (IC50: 8 nM).

MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of S

CGP52411 is an orally active, and ATP-competitive inhibitor of EGFR (IC50: 0.3 μM). CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells and dramatically inhibits and reverses the formation of β-amyloid Aβ42 fibril aggregates. CGP52411 can be used in studies about Alzheimer's diseases.

CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).

WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170

Olomoucine is an ATP competitive inhibitor of Cdk2/cyclin A, Cdc2/CyclinB, CDK2/CyclinE, CDK5/p35, and ERK1/p44 MAP kinase with IC50s of 7, 7, 7, 3 and 25 µM, respectively. Olomoucine regulates cell cycle and exhibits anti-melanin tumor activities.

BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with IC 50 of 0.3 nM. BLU2864 exhibits anti-tumor activity. BLU2864 has potential to be used in cancer and polycystic kidney disease research [1] [2].

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively).

NVS-PAK1-1 is a potent allosteric inhibitor of PAK1 with an IC 50 of 5 nM for dephosphorylated PAK1 and 6 nM for phosphorylated PAK1 as assessed. Inhibition is ATP-competitive, most likely due to indirect competition due to incompatibility of ATP binding with the DFG-out binding conformation of the allosteric compound. NVS-PAK1-1 has an IC50 of 270 nM against dephosphorylated PAK2 and 720 nM against phosphorylated PAK2 respectively [1].

Plogosertib (CYC140) is an orally active, selective, potent, and ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib exhibits antiproliferative and anticancer activity and can be used for the study of solid and hematologic tumors. and hematologic tumors.

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).

RO9021 is an orally bioavailable, novel ATP-competitive SYK inhibitor (average IC50: 5.6 nM).