adamts-5 inhibitor

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.

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.

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.

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).

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

KRAS G12D inhibitor 5 is a KRAS G12D inhibitor for the potential treatment of pancreatic cancer.

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].

ADAMTS-5-IN-2 is a potent inhibitor of ADAMTS-5, exhibiting an IC50 of 0.71 µM, and holds potential for osteoarthritis research.

ADAMTS-5-IN-3 (Example 37-2) is a potent inhibitor of ADAMTS-5 (IC50: 8 nM) and ADAMTS-4 (IC50: 12 nM).ADAMTS-5-IN-3 can be used to study diseases associated with cartilage degeneration or disruption of cartilage homeostasis, particularly osteoarthrosis and/or rheumatoid arthritis.

Topoisomerase II inhibitor 5 (Compound E24) is a DNAtopoisomerase II inhibitor with anticancer effects.

Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1].

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

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

P-gp inhibitor 5 is a potent inhibitor of P-glycoprotein (P-gp), inhibiting P-gp by a factor of 2.5 and 3.0 at 1.25 μM and 2.5 μM, respectively. p-gp inhibitor 5 exhibits anti-proliferative effects on some cancer cells. P-gp inhibitor 5 was able to restore cellular sensitivity to Vincristine and Paclitaxel, thereby 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.

Pim-1 kinase inhibitor 5 (Compound 4c), with an IC50 of 0.61 μM, exhibits cytotoxicity against various cancer cell lines, including 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].

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

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 inhibitor of HIF-1, exhibiting an IC50 value of 2.38 μM and demonstrating significant anti-angiogenic potential [1].

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

ITK inhibitor 5 (compound 27) is a highly potent and selectively targeted inhibitor of ITK. It exhibits IC50 values of 5.6 nM and 25 nM for ITK and BTK respectively [1].

KRAS G12C inhibitor 5 is a KRas G12C inhibitor.

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) serves as a potent regulator of tumor immunity by inhibiting RIP1, functioning similarly to SIR1-365 (compound 13) in suppressing necrosis and ferroptosis [2].

GLS1 Inhibitor-5 (compound 24y) is a selective, orally active inhibitor of glutaminase 1 (GLS1) (IC50: 68 nM). gLS1 Inhibitor-5 induces apoptosis and exhibits anti-tumour 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 inhibitor of glyoxalase I (Glo-I), with an IC50 value of 1.28 μM. This compound holds promise as an anticancer agent [1].

ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. ERK1/2 inhibitor 5 has the potential to investigate or prevent cancer, inflammation or other proliferative diseases.

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

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].

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 IC 50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for venous thromboembolism research[1].

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

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

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. It exhibits a substantial cytotoxic effect on NCI-H460 cells, with an IC50 value of 154.5 nM. Moreover, this compound demonstrates excellent cell permeability [1].

T-5224 is a transcription factor c-Fos/AP-1 inhibitor, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors.

Aldumastat (GLPG1972) is a highly potent, specific and orally active inhibitor of ADAMTS-5.Aldumastat is used for the study of osteoarthritis of the knee.