kdm-5-inhibitor

5-LOX inhibitor (1-(sec-Butyl)-4-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one) is one of the impurities of itraconazole, a selective LOX-5 inhibitor.

GSK-3 Inhibitor 5 (4-Cyanophenacyl bromide) is a ketone derivative that is used as an intermediate in pharmaceuticals and organic synthesis, and inhibits glycogen synthase kinase 3 (GSK-3).

1-[4-(2,3-dihydro-1,4-benzodioxine-6-sulfonyl)piperazin-1-yl]-2-(6-methyl-1-benzofuran-3-yl)ethan-1-one Yes An organic structural unit.

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor (IC50: 15.3 nM) that reduces CCl4-induced hepatic fibrosis and exhibits anti-hepatic fibrosis effects.

Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer properties.

Topoisomerase I inhibitor 5 is an efficient topoisomerase I inhibitor with an IC50 value, effectively disrupting DNA and inhibiting topoisomerase I activity. It induces apoptosis in MCF-7 cells and arrests the cell cycle at the G1 phase, displaying potency in reversing P-gp-mediated resistance to Adriamycin [1].

Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue and anti-tuberculosis agent with no apparent cytotoxicity.

Protein kinase inhibitor 5 is a potent inhibitor of TRK-A, with an IC50 of 1.8 nM, and effectively suppresses cell viability [1].

P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor, reducing P-gp activity by a factor of 2.5 and 3.0 at 1.25 μM and 2.5 μM, respectively. It exhibits anti-proliferative effects on certain cancer cells and restores cellular sensitivity to Vincristine and Paclitaxel, reversing the multidrug resistant (MDR) phenotype of ABCB1 Flp-InTM-293 and KBvin.

SIRT5 Inhibitor 5 is a potent substrate-competitive inhibitor of SIRT5, exhibiting an IC50 of 0.21 µM, and does not interact with the NAD+-binding pocket [1].

Chitin synthase inhibitor 5 effectively blocks chitin synthase, a key enzyme in fungal cell wall formation, with a low IC50 value of 0.14 mM. Chitin synthase inhibitor 5 demonstrates broad-spectrum antifungal activity against Candida albicans, Aspergillus species, and Cryptococcus neoformans.

KRAS G12D inhibitor 5 is a potential treatment for pancreatic cancer that targets the KRAS G12D mutation.

WIN site inhibitor 1 TFA is a WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5) inhibitor (Kd: 0.1 nM).

Pim-1 kinase inhibitor 5 (Compound 4c) has an IC50 of 0.61 μM and exhibits cytotoxicity against cancer cell lines HepG2, MCF-7, PC3, and HCT-116, with IC50 values ranging from 6.95 to 20.19 μM [1].

Protein kinase inhibitor 5 sulfate hydrate, a potent TRK-A inhibitor, exhibits an IC50 of 1.8 nM and impairs cell viability [1].

c-Myc Inhibitor 5 (DA3) is a fluorescent bispurine compound with a long-chain bridge that selectively binds to the c-MYC G-quadruplex, exhibiting a dissociation constant (K D) of 16 μM. Unlike other G4-driven oncogenes, this inhibitor specifically suppresses c-MYC expression [1].

HIF-1 inhibitor-5 (Compound 16e) is a potent HIF-1 inhibitor with an IC50 value of 2.38 μM, demonstrating significant anti-angiogenic potential [1].

IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor with an IC50 of 64.4 nM for MOG cells and an IC50 of 34.9 nM for wild-type IDH1 glioma cells expressing exogenous mutant IDH1 R132H protein.

ITK inhibitor 5 (compound 27) is a highly potent and selective ITK inhibitor, demonstrating IC50 values of 5.6 nM for ITK and 25 nM for BTK [1].

KRAS G12C inhibitor 5 is a KRas G12C inhibitor. (Add a sentence that describes its primary function, mechanism, or application.)

WRN Inhibitor 5 (Example 157), a cyclic vinyl sulfone-based compound, serves as an inhibitor of Werner Syndrome ATP-dependent helicase enzyme (WRN). It is utilized in cancer research [1].

ERK1 2 inhibitor 5 is a potent inhibitor of ERK1 2, with potential applications in investigating or preventing cancer, inflammation, and other proliferative diseases.

Carbonic anhydrase inhibitor 5 is a potent and selective inhibitor of human carbonic anhydrase (hCA), targeting hCA II (IC50: 42.9 nM), hCA IX (IC50: 47.6 nM), and hCA XII (IC50: 6.7 nM).

URAT1 Inhibitor 5 (compound 16) serves as a powerful inhibitor of URAT1 and is utilized in hyperuricemia research [1].

RIP1 kinase inhibitor 5 (example 1) is a potent regulator of tumor immunity, inhibiting RIP1 and similarly to SIR1-365 (compound 13), suppresses necrosis and ferroptosis [2].

GLS1 Inhibitor-5 (compound 24y) is a selective, orally active glutaminase 1 (GLS1) inhibitor (IC50: 68 nM) that induces apoptosis and exhibits anti-tumor effects.

Glutaminyl Cyclase Inhibitor 5 is a potent, selective inhibitor of human glutaminyl cyclase (hQC), demonstrating an inhibition concentration half-max (IC 50) of 3.2 nM.

PI3K/mTOR Inhibitor-5 is a potent dual inhibitor of PI3K and mTOR, displaying IC50 values of 86.9 nM (for PI3K) and 14.6 nM (for mTOR), respectively.

Glyoxalase I inhibitor 5 (Compound 9h) is a potent glyoxalase I (Glo-I) inhibitor with an IC50 of 1.28 μM, showing potential as an anticancer agent [1].

PKI PKA Inhibitor (5-24) is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki= 2.3 nM) derived from the active site of the skeletal muscle inhibitor protein.1It mimics the protein substrate by binding to the catalytic site through the arginine-cluster basic subsite.1The prominent enzyme-substrate interaction site occurs where PKA catalytic subunit residues Tyr235and Phe239form a sandwich-like structure with residue Phe10of PKI (5-24).2

Microtubule inhibitor 5 (compound 17f) is a highly potent cytotoxic agent that inhibits microtubule function, exhibiting a substantial cytotoxic effect on NCI-H460 cells with an IC50 value of 154.5 nM. Additionally, this compound demonstrates excellent cell permeability [1].

α-Synuclein inhibitor 5 is a potent inhibitor of α-Synuclein (α-Syn) aggregation across the blood-brain barrier (IC50: 1.22 μM), with 94.3% inhibition at 30 μM.

ChoKα Inhibitor-5, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoKα1 with an IC50 value of 0.64 μM and induces apoptosis. It is utilized in cancer research [1].

ADAMTS-5 Inhibitor is an inhibitor of ADAMTS-5 with an IC50 of 1.1 µM and can be used in studies about cartilage destruction in arthritis.

sEH inhibitor-5 is a potent inhibitor of sEH (soluble epoxide hydrolase) (IC50: 0.1 nM).

Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor with IC50 values ranging from 0.1 μM to 1 μM, suitable for venous thromboembolism research[1].

FAK inhibitor 5 is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.

PI3Kγ inhibitor 5 is a potent inhibitor of phosphoinositide 3-kinase γ (PI3Kγ), exhibiting an exceptional IC50 value of 34 nM.

CPI-455 analogue (CPI-455 analogue) is an analogue of CPI-455 which is a KDM5 inhibitor.

KDM5-C70 is an ethyl ester derivative of KDM5-C49 and functions as an effective, cell-permeable, pan-KDM5 histone demethylase inhibitor. It exhibits an antiproliferative effect in myeloma cells and induces a genome-wide elevation of H3K4me3 levels.

KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.