pde9 inhibitor

Topoisomerase I Inhibitor 9 (compound 3d), a specific inhibitor of leishmanial topoisomerase IB, exhibits antileishmanial activity, demonstrating an IC50 value of 34.81μM against L. donovani promastigotes [1].

PDE-9 inhibitor is used for treatment neurodegenerative diseases.

SIRT5 inhibitor 9 (compound 14), with an IC50 of 4.07 μM, is a competitive inhibitor of the sirtuin SIRT5, exhibiting potential anticancer properties [1].

Bromodomain inhibitor-9 is an inhibitor of Bromodomains that selectively inhibits the activity of BRD4-1 with a Kd value of 12 nM. Bromodomain inhibitor-9 can be used in studies of diseases related to systemic or lipid metabolism, tissue inflammation, fibrosis, or chronic autoimmune diseases.

MNK Inhibitor 9 is a potent, selective inhibitor of MNK1/2, demonstrating IC50 values of 0.003 µM for both MNK1 and MNK2. It exhibits good cell permeability, making it suitable for tumor-related research.

CypD inhibitor C-9 is a CypD inhibitor, it attenuates mitochondrial and cellular perturbation insulted by Aß and calcium stress.

FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor with potent binding affinity, exhibiting an IC50 of 0.85 nM. It targets the ATP-binding pocket of FGFR1 and demonstrates anticancer activity [1].

c-Myc Inhibitor 9 (Compound 332) is an effective c-Myc inhibitor, exhibiting a logEC50 of ≥6, and demonstrating significant tumor growth inhibition in nude mouse models. This compound is utilized in cancer research.

Carbonic anhydrase inhibitor 9 is a potent inhibitor of carbonic anhydrase (CA) that acts on hCA II (Ki: 56.4 nM) and IX (Ki: 56.9 nM) and exhibits antiproliferative effects.

HIV-1 inhibitor-9 exhibits potent inhibition activity at low nanomolar concentrations against both the wild-type (WT) HIV-1 strain and multiple strains that have developed resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs).

ProMMP-9 inhibitor-3c is a potent and specific proMMP-9 inhibitor which disrupts f MMP-9 homodimerization and prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR.

PI3K/mTOR Inhibitor-9 (Compound 1) is a potent inhibitor of both mTOR and PI3K, acting on mTOR (IC50: 38 nM), PI3Kα (IC50: 6.6 nM), PI3Kγ (IC50: 6.6 nM) and PI3Kδ (IC50: 0.8 nM).

α-Synuclein inhibitor 9 (Compound 20C) is a molecule that targets and binds to cavities within mature α-synuclein fibrils, diminishing their β-sheet content. It effectively inhibits the aggregation of A53T α-synuclein and exhibits neuroprotective properties, enhancing brain functionality and alleviating motor impairments. This compound is utilized in research related to Parkinson's disease (PD). [1]

ATM Inhibitor-9 (Compd 7a) is a potent inhibitor of ATM kinase, exhibiting an IC50 value of 5 nM, and is utilized in cancer research [1].

Tuberculosis inhibitor 9 (compound 3d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and Mycobacterium marinum, with an MIC 90 of 0.64 μM for both organisms [1].

MMP-2/MMP-9-IN-1 is a potent, highly selective and orally bioavailable inhibitor of type IV collagenases (MMP-9 and MMP-2) with an IC50 of 0.24 and 0.3 1 μM for MMP-9 and MMP-2, respectively. activity, which can be used to study cancer.

Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B bipolar kinase inhibitor, acting on Aurora A (IC50: 0.093 μM), Aurora B (IC50: 0.09 μM). broad-spectrum anti-proliferative activity.

Mcl-1 Inhibitor 9 (Example 2) is a potent inhibitor of myeloid cell leukemia 1 (Mcl-1), demonstrating anti-tumor activity with an IC50 value of 0.21889 nM.

Chitin synthase inhibitor 9 is a chitin synthase (CHS) inhibitor that exhibits broad-spectrum antifungal activity and can be used in studies of fungal infections.

MMP-9/MMP-13 Inhibitor I is a dual inhibitor of MMP-9 and MMP-13 with IC50 of both 0.9 nM. MMP-9/MMP-13 Inhibitor I is over 20 times more selective for MMP-9/MMP-13 than other MMPs.

ERK1/2 Inhibitor 9 (Probe 1), a covalent antagonist of ERK1/2, exhibits sub-micromolar efficacy in cellular assays (A375 GI50=0.47 μM) and facilitates the reduction of phospho-ERK1/2 levels. When conjugated with trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine-tagged Thalidomide), it forms the corresponding ERK-CLIPTAC, promoting targeted ERK1/2 degradation [1].

HIV-1 integrase inhibitor 9 (compound 8a) is a potent inhibitor of HIV-1 RNase H (IC50: 12.3 μM) and has antiviral effects.

MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). It also decreases the activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells when used at concentrations of 50 and 100 μM.

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.

KRAS inhibitor-9 (DUN09716) is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSC-LC cells with KRAS mutation but not normal lung cells

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).

Topoisomerase II inhibitor 9 is a Topo II inhibitor (IC50: 0.97 μM) and DNA embedding agent (IC50: 43.51 μM) that blocks the Hep G-2 cell cycle in the G2/M phase and induces apoptosis.

KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. Among them, the RAS protein family is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 shows research potential for KRAS G12D-mediated cancer.

Caspase-9 Inhibitor III (Ac-LEHD-cmk), a caspase-9 inhibitor, exhibits protective effects against ischemia-reperfusion-induced myocardial injury.

PDE9-IN-(S)-C33 ((S)-C33) is a potent and selective inhibitor of PDE9 (IC50 = 11 nM). PDE9-IN-(S)-C33 can be used for central nervous system diseases and diabetes research.

PDE9-IN-1 is a selective and orally bioavailable Inhibitor of PDE9A(IC50 of 8.7 nM).

PDE11A4-IN-1 (compound 23b) is a potent, selective inhibitor of PDE11A4, demonstrating an IC50 of 12 nM and exhibiting high selectivity against PDE1, PDE2, PDE7, PDE8, and PDE9 [1].

Tovinontrine (IMR-687) (IMR-687) is a potent and selective inhibitor of phosphodiesterase-9 (PDE9), designed to target sickle cell disease treatment. It exhibits high efficacy, with IC 50 values of 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively [1].

(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine, serves as a potent inhibitor of phosphodiesterase 9 (PDE9) with an inhibition concentration (IC50) of 0.041 μM, primarily utilized in the research of neurological diseases [1].

Irsenontrine (E2027) maleate is a selective and orally active inhibitor of phosphodiesterase 9 (PDE9). It can be utilized in the study of neurological diseases.

IMR687 is a PDE9 inhibitor that slows or stops the hydrolysis of cGMP. IMR687 can be regarded as a highly promising drug against Alzheimer's for improving memory.

Irsenontrine (E2027) is a selective and orally active inhibitor of phosphodiesterase 9 (PDE9), primarily used for researching neurological diseases.