atx inhibitor 7

ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.

URAT1 inhibitor 7 is a novel and potent inhibitor of the human uric acid transporter protein URAT1 (IC50:12 nM).URAT1 inhibitor 7 inhibits CYP2C9 with an IC50 of 4.2 μM.URAT1 inhibitor 7 can be used to study hyperuricemia and gout.

C-Myc Inhibitor 7, serving as both a c-Myc inhibitor and a multi-target protein degrader, effectively degrades proteins c-MYC, CK1α, GSPT1, and IKZF1/2/3 across various tumor cell types. It holds potential for research into diseases associated with high c-Myc expression, including cancer, cardiovascular and cerebrovascular conditions, and viral infections.

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,.

PI3Kα Inhibitor 7 is a useful organic compound for research related to life sciences. The catalog number is T9312 and the CAS number is 1239978-63-2.

KRAS G12D inhibitor 7, is a highly potent inhibitor specifically targeting KRAS G12D.

Protein kinase inhibitor H-7 (5-(2-methylpiperazine-1-sulfonyl)isoquinoline) is a potent inhibitor of protein kinase C (PKC) with a Ki of 6 μM. Protein kinase inhibitor H-7 is also a cyclic nucleotide dependent protein kinase inhibitor.

ATX inhibitor 1 is a potent ATX inhibitor (IC50: 1.23 nM, FS-3 and 2.18 nM, bis-pNPP).

ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) (IC50: 218.9 μM) that lacks inhibitory activity against LPAR1.

PI3K/mTOR Inhibitor-7 is a potent dual PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-7 is 4.7-fold more potent than gedatolisib, with IC50 values of 1.4 μM and 0.3 μM, respectively. 10 μM of PI3K/mTOR Inhibitor-7 is able to significantly inhibit the PI3K/Akt/mTOR signalling pathway. PI3K/mTOR Inhibitor-7 has shown potential for research in cancer diseases.

Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants.

ATX inhibitor 14, an indole-based carbamate derivative, is a potent inhibitor (IC50: 0.41 nM) of self-adhesive proteins (ATX) and has shown potential for research in fibrosis-related diseases.

Protein kinase inhibitor H-7 dihydrochloride(H-7 dihydrochloride) is a potent protein kinase C (PKC) inhibitor. Protein kinase inhibitor H-7 dihydrochloride (100 μM) significantly inhibits TPA (skin tumor promoter, 12-O-tetradecanoylphorbol-13-acetate) and phospholipase C-induced ODC (ornithine decarboxylase) inhibited PMA-induced promiscuity cell lysis activity.

Chitin synthase inhibitor 7 (compound 9c) is a potent inhibitor of chitin synthase (CHS) (IC50: 0.37 nM). synthase inhibitor 7 can be used to study fungal infections.

ATX inhibitor 19 is a potent inhibitor of ATX (IC50: 156 nM).

ATX inhibitor 12 is an orally active ATX inhibitor (IC50: 1.72 nM). In C57Bl/6J mice, oral administration of ATX inhibitor 12 at a dose of 60 mg/kg was effective in inhibiting structural lung damage and reducing fibrotic lesions.

FGFR1 Inhibitor 7 (compound 5), a potent FGFR1 tyrosine kinase inhibitor, exhibits an IC50 of 0.33 nM against its target and demonstrates broad-spectrum cytotoxicity against human cancer cell lines. Additionally, it inhibits MOLT3 cells with an IC50 of 2.1 μM [1].

Tuberculosis inhibitor 7 (compound 2d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and Mycobacterium marinum, with both displaying a MIC 90 of 0.63 μM [1].

ERK1/2 inhibitor 7 is a potent inhibitor of ERK, acting on ERK2 (IC50: 0.94 nM).

GSK-3β inhibitor 7 is a GSK-3β inhibitor (IC50: 5.25 μM). GSK-3β inhibitor 7 acts by inserting into the ATP-binding binding pocket of GSK-3β and forming hydrogen bonds. GSK-3β inhibitor 7 has a high rate of glucose uptake by hepatocytes ( 83.5%) and can be used to study a variety of diseases such as cancer, diabetes, inflammation, Alzheimer's disease and bipolar disorder.

Tubulin inhibitor 7 is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines (tubulin polymerization (IC50: 0.52 μM), K562 cell growth (IC50: 11 nM)).

α- Synuclein inhibitor 7 (compound 3gf) is effective α- Synuclein ( α- Syn) aggregation inhibitor, IC50 is 1.95 μM, inhibition rate at 30μM was 85.8%. α- Synuclein inhibitor 7 has blood-brain barrier permeability.

Glyoxalase I inhibitor 7 (Compound 6) is a potent inhibitor of glyoxalase I (Glo-I) with an IC50 of 3.65 μM. It exhibits potential as an anticancer agent [1].

ATX inhibitor 11 is a potent inhibitor of ATX (autotaxin) (IC50: 2.7 nM). ATX inhibitor 11 alleviates the severity of fibrotic tissue and effectively reduces the deposition of α-SMA, a biomarker of fibrosis, in a mouse model of fibrosis. ATX inhibitor 11 can be used to study lung fibrosis.

ATX inhibitor 21 is a potent inhibitor of ATX (IC50: 3490 nM).

PI3Kγ Inhibitor 7 (compound 2) is a potent, orally active agent that selectively inhibits PI3Kγ with an IC50 of 3.42 nM and demonstrates antitumor activity [1]. It also exhibits varying inhibitory effects on other PI3K isoforms, with IC50 values of 4768 nM for PI3Kα, 878.1 nM for PI3Kβ, and 355.2 nM for PI3Kδ.

ATX inhibitor 20 is a potent inhibitor of ATX (IC50: 2.3 nM).

Compounds 17o (IC50= 14.0 nM, NCI-H460) and 17p (IC50= 2.9 nM, NCI-H460) with furan moieties show potent nanomolar levels of cytotoxic activity against various human cancer cell lines.

Topoisomerase II inhibitor 7, a potent inhibitor of the topoisomerase II alpha subtype, exhibits an IC50 of 3.19 μM. It effectively induces cell cycle arrest and apoptosis.

IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC 50 of less than 100 nM .

ATX inhibitor 15 (compound 30) is an indole-based carbamate derivative with a strong inhibitory effect on autotaxin (ATX), demonstrated by an IC50 of 2.17 nM. Additionally, ATX inhibitor 15 effectively inhibits ATX activity in vivo and suppresses the expression of pro-fibrotic genes. Furthermore, ATX inhibitor 15 exhibits protective effects in lung fibrosis induced by Bleomycin in mice [1].

KRAS inhibitor-7 is a potent KRAS G12C inhibitor.

ATX inhibitor 8 is an inhibitor of the autocrine motor factor Autotaxin (ATX).

Carbonic anhydrase inhibitor 7 is a potent inhibitor of human carbonic anhydrase (hCA), acting on hCA IX (Ki: 6.5 nM), hCA II (Ki: 7.1 nM), hCA XII (Ki: 72.1 nM) and hCA I (Ki: 255.8 nM).

sEH inhibitor-7 is a soluble epoxide hydrolase (sEH) inhibitor that inhibits sEH in human and mouse with IC 50 s of 6.2 μM and 0.15 μM, respectively. sEH inhibitor-7 is associated with anti-inflammatory active molecules.

GLS1 Inhibitor-7 (compound 4d) serves as a GLS1 antagonist with an IC50 value of 46.7 μM, demonstrating potential applications in anticancer, antiaging, and antiobesity therapies [1].

RAS inhibitor Abd-7 is a powerful compound (Kd=51 nM) that binds to RAS and inhibits the protein-protein interaction (PPI) between RAS and its effectors. By interacting with RAS within cells, RAS inhibitor Abd-7 hinders RAS-effector interactions and suppresses endogenous RAS-dependent signaling. Additionally, RAS inhibitor Abd-7 disrupts the PPI of different mutant KRAS proteins with PI3K, CRAF, RALGDS, as well as NRAS Q61H and HRAS G12V[1].

JNK3 inhibitor-7, a potent and orally active compound that can cross the blood-brain barrier, acts as a JNK3 inhibitor with IC50 values of 53 nM for JNK3, 973 nM for JNK2, and 1039 nM for JNK1. Demonstrating significant neuroprotective effects, JNK3 inhibitor-7 holds potential for Alzheimer’s disease (AD) research [1].

ATX inhibitor 13 (compound 10c) is an orally active ATX inhibitor (IC50: 3.4 nM). ATX inhibitor 13 is capable of blocking the cell cycle of RAW264.7 cells in the G2 phase, inhibiting cell proliferation and migration and inducing apoptosis. ATX inhibitor 13 exhibited an inhibitory effect on tumour colony formation.

ATX inhibitor 9 is a thickened heteroaryl derivative compound and a potent inhibitor of ATX. Among them Autotaxin (ATX), also known as ENPP2, is a secreted enzyme highly expressed mainly in lung cancer cells, bronchial epithelial cells and alveolar macrophages.ATX inhibitor 9 has research potential for cancer or fibrous degenerative diseases.

RIP1 Kinase Inhibitor 7 (Compound 41) serves as a potent inhibitory agent for receptor interacting protein 1 kinase (RIP1) with an IC50 of under 100 nM. Additionally, it demonstrates an EC50 ranging from 1 to 100 nM in cell necrosis assays [1].

SIRT5 inhibitor 7 (compound 58), a selective and substrate-competitive SIRT5 inhibitor, exhibits anti-inflammatory properties by modulating protein succinylation and attenuating pro-inflammatory cytokine release. It demonstrates renal protective effects and is active in vivo, showing efficacy in AKI mouse models subjected to lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury [1].

Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound can prevent endothelial cell tube formation and aberrant vessel growth in a rat model of Matrigel-induced choroidal neovascularization.

HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor (IC50: 33.3 nM).

ATX inhibitor 17, a powerful ATX inhibitor, exhibits an IC50 value of 0.019 µM, demonstrating significant anti-proliferative effects in breast cancer cells.

ATX inhibitor 16 is a potent inhibitor of ATX (IC50: 0.0021 μM). ATX inhibitor 16 exhibits a significant anti-proliferative effect on breast cancer cells.

ATX inhibitor 10 is a nitrogen-containing heterocyclic compound that is a potent inhibitor of ATX. Among other things, ATX plays a role in causing pathologies including fibrosis, neurodegeneration, arthritis, neuropathic pain, and cancer. ATX inhibitor 10 has shown research potential for ATX-related diseases.