set7 inhibitor

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.

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.

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.

Arginase Inhibitor 7 (compound A17), an inhibitor of arginase (ARG1), exhibits an IC 50 value of 0.16 μM and possesses high oral bioavailability [1].

WRN inhibitor 7 (Compound h6), a potent inhibitor of Werner syndrome helicase, demonstrates effective suppression of WRN's helicase and ATPase activities with IC50 values of 9.8 μM and 15.8 μM, respectively. This compound is utilized in the study of microsatellite instable (MSI) cancers [1].

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 Topoisomerase I inhibitor that significantly reduces tumor growth by up to 79% and extends the lifespan of mice bearing P388 lymphoma transplants by 153%.

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), a potent inhibitor of chitin synthase (CHS) with an IC50 of 0.37 nM, can be used to study fungal infections.

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

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, with an IC50 of 0.94 nM for ERK2.

GSK-3β inhibitor 7 is a GSK-3β inhibitor (IC50: 5.25 μM) that acts by inserting into the ATP-binding pocket of GSK-3β and forming hydrogen bonds. It exhibits a high rate of glucose uptake by hepatocytes (83.5%) and can be used to study various 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 glyoxalase I (Glo-I) inhibitor with an IC50 of 3.65 μM, exhibiting potential as an anticancer agent [1].

ATX inhibitor 7 is an autotaxin inhibitor that demonstrates good oral exposure.

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.

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

KRAS inhibitor-7 is a potent inhibitor of KRAS G12C. (KRAS inhibitor-7 specifically targets the G12C mutation in KRAS, a protein involved in cell signaling and cancer development.) [KRAS inhibitor-7 exhibits high binding affinity and selectivity for the mutant KRAS protein.]

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) is a GLS1 antagonist with an IC50 value of 46.7 μM, showing 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].

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].

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].

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 inhibitor of HIV-1 integrase (IC50: 33.3 nM).

Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin is a SET7 9 inhibitor and ameliorates renal fibrosis by inhibiting H3K4 methylation.

DC-S239 (DC-S239) is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with anticancer activity.

CARM1-IN-1 (CARM1-IN-7G) is a selective inhibitor of CARM1 with IC50 of 8.6 μM. CARM1-IN-1 shows weak activity against PRMT1 and SET7 with IC50 > 600 μM.

CARM1-IN-1 hydrochloride is a potent and selective inhibitor of CARM1 (IC50: 8.6 μM) with minimal inhibition of PRMT1 and SET7.

DC-S238 is a potent and selective histone methyltransferase SET7 inhibitor.

Setin-1 is the most potent Set7 inhibitor that acts by inhibiting the KMTase G9a.

Epigenetic Multiple Ligand is a cell-permeable inhibitor of substrate processing by several chromatin-associated enzymes, including SIRT1/2, H3/SET7, H3/p300/CBP, H4/RmtA, PABP1/CARM1, and H4/PRMT1. It acts by inducing either apoptosis or granulocytic differentiation.

DC-S100 is a selective histone methyltransferase SET7 inhibitor.