non-atp competitive inhibitor

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

ATP synthase inhibitor 1 is an inhibitor of the c subunit of the F1/FO-ATP synthase complex. It inhibits mitochondrial permeability transition pore (mPTP) opening and does not affect ATP levels.

ATP Synthase Inhibitor 2 (Compound 22) TFA is a potent inhibitor of Pseudomonas aeruginosa ATP synthase with an IC50 value of 10 μg/mL. It effectively halts ATP synthesis in Pseudomonas aeruginosa at a concentration of 128 μg/mL [1].

BRM/BRG1 ATP Inhibitor-4, a potent inhibitor of BRG1/BRM, is utilized in the research of cancers and BAF complex-related disorders.

ATP Synthase Inhibitor 2, a compound targeting Pseudomonas aeruginosa (PA) ATP synthase with an IC50 of 10 μg/mL, fully inhibits the ATP synthesis activity of PA at a concentration of 128 μg/mL [1].

BRM BRG1 ATP Inhibitor-2 is a BRG1 BRM ATPase inhibitor, suitable for studies on the treatment of BAF-related disorders.

BRM BRG1 ATP Inhibitor-3 is a potent inhibitor targeting both BRM and BRG1 components of the BAF complex, with IC50 values of 10.4 nM for BRM and 19.3 nM for BRG1, and holds potential for research in cancer and BAF complex-related disorders.

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.

Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1 2 expression and inducing apoptosis.

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

Selumetinib (AZD6244) is a MEK1 2 inhibitor that inhibits MEK1 (IC50=14 nM) with potent selectivity and is non-ATP-competitive. Selumetinib has antitumor activity and is used for the treatment of neurofibromatosis type 1 (NF1).

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

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.

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

MK-8033 hydrochloride is an effective and orally active dual inhibitor of ATP competitive c-Met/Ron, with 1 nM for c-Met and 7nM for Ron IC50. MK-8033 hydrochloride has a high affinity for activated kinase conformation, and is suitable for the study of breast cancer, bladder cancer, and non-small cell lung cancer (NSCLC).

Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1 2 (IC50: 0.07 0.06 μM).

Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.

Butyrolactone I (Olomoucin) is an ATP-competitive inhibitor of CDK and cdc2 kinase family. Butyrolactone I shows antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines.

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1 2 inhibitor (IC50: 17 nM).

AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

MK2-IN-1 hydrochloride (MK 25) is a highly selective, non-ATP competitive inhibitor of p38/mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2, IC50: 0.11 μM) [1].

Rigosertib sodium (ON-01910), a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.

LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM and acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. Additionally, LX2343 stimulates autophagy, promoting Aβ clearance.

SKI II (SphK-I2) is a highly selective and non-ATP-competitive S1P receptor inhibitor (IC50: 0.5 μM) while exhibiting no inhibitory action on other kinases including PKCα, PI3K, and ERK2.

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.

CMPD1 is a non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor(apparent Ki (Kiapp): 330 nM).

PD318088 is a non-ATP competitive allosteric MEK1 2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

GSK3-IN-3 is a mitochondrial autophagy (mitophagy) inducer and GSK-3 inhibitor (IC50: 3.01 μM) that induces parkin-dependent mitochondrial autophagy. GSK3-IN-3 is non-ATP and non-substrate competitive and neuroprotective against 6-OHDA.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

MK1496 is a n orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

OXA-06 hydrochloride, an ATP-competitive ROCK inhibitor, impedes anchorage-dependent growth and invasion in non-small cell lung cancer cell lines. It effectively inhibits cofilin phosphorylation without inducing apoptosis [1].

Poloxime is a hydrolysis product of poloxin and is a non-ATP-competitive Plk1 inhibitor. It also has moderate Plk1 inhibitory activity.

RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a broad spectrum of tumor models. RO4927350 inhibits not only ERK1/2 but also MEK1/2 phosphorylation. In cancer cells, high basal levels of phospho-MEK1/2 rather than phospho-ERK1/2 seem to correlate with greater sensitivity to RO4927350. Furthermore, RO4927350 prevents a feedback increase in MEK phosphorylation, which has been observed with other MEK inhibitors. RO4927350 represents a novel therapeutic modality in cancers with aberrant MAPK pathway activation.

Tripolin A is a specific non-ATP competitive inhibitor of Aurora A kinase(Aurora A and Aurora B with IC50 values of 1.5 μM and 7 μM, respectively)

KIF18A-IN-4 is a moderately potent, non-competitive KIF18A inhibitor of ATP and microtubule with an IC50 of 6.16 μM. It selectively acts on many mitotic kinesins and kinases, without directly affecting microtubule protein assembly, and shows anti-tumour effects.

ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I.

Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase Akt pathway, promotes histone H2AX phosphorylation, and induces G2 M arrest in the cell cycle.

GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic properties.

Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).

ON-01910 is a non-ATP-competitive PLK1 inhibitor(IC50 of 9 nM, in a cell-free assay). It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells.It is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity.

MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, selectively inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It induces apoptosis and arrests the cell cycle in HepG2 cells, demonstrating strong antitumor effects against various human cancer cell lines, thereby highlighting its significance for cancer research [1].

Miransertib mesylate is a selective AKT inhibitor that binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may result in reduction in tumor cell proliferation and the induction of tumor cell apoptosis.

IPA-3 is a selective, non-ATP competitive Pak1 inhibitor with an IC50 of 2.5 μM, and it does not inhibit group II PAKs (PAKs 4-6).

Selumetinib (AZD6244) is a potent, selective, non-ATP-competitive MEK1/2 inhibitor that inhibits MEK1/2 phosphorylation levels with an IC50 value of 14 nM for MEK1.