caspase-9 inhibitor iii

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

Cdk1 2 Inhibitor III is a selective inhibitor of Cdk1 2 with an IC50 value of 2.1 μM against CDK1 cyclin B.

9-dihydro-13-acetylbaccatin III (9-DHAB III)is an apoptosis inducer. It shows cytotoxicity against the MCF7 cell line and drug-resistant cell line MCF7-ADR.

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) (PIK-III analogue) is a potent and selective inhibitor of VPS34( IC50 : 15 nM)

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

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].

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].

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.

Z-DEVD-FMK, a Caspase-3 Inhibitor, is an irreversible, cell-permeable inhibitor of caspase-3/CPP32 that impedes tumor cell apoptosis. In vivo studies show it offers neuroprotection in rat hippocampi post-seizures and considerably diminishes post-traumatic apoptosis, enhancing neurological recovery in rats before and after traumatic brain injury induction.

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.

HSP47 inhibitor III suppressed collagen type I expression in human and mouse cells and suppressed the viability and migration of lung fibroblasts.

Ftase Inhibitor III, derived from a phenotypic screen, functions as an anion-dependent inhibitor of Farnesyltransferase.

Human PD-L1 inhibitor III [Human PD-L1 inhibitor] is a bioactive compound designed to inhibit the programmed death-ligand 1 (PD-L1) protein in humans.

KRAS G12D inhibitor 9 is a potent agent targeting KRAS G12D, an important member of the RAS protein family involved in intracellular signaling crucial for growth and development. This inhibitor shows significant research potential for KRAS G12D-mediated cancer.

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].

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.

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

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

MMP-2 MMP-9-IN-1 is a potent, highly selective, and orally bioavailable inhibitor of type IV collagenases [MMP-9 and MMP-2], exhibiting IC50 values of 0.24 μM for MMP-9 and 0.31 μM for MMP-2, which can be used to study cancer.

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

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

Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA B bipolar kinase inhibitor with an IC50 of 0.093 μM for Aurora A and 0.09 μM for Aurora B, demonstrating broad-spectrum anti-proliferative activity.

Chitin synthase inhibitor 9, a chitin synthase (CHS) inhibitor, exhibits broad-spectrum antifungal activity and is useful for studies of fungal infections.

Lck Inhibitor III, a potent inhibitor of Lck, exhibits an IC50 value of 867 nM. Additionally, this compound effectively inhibits IL-2 synthesis in Jurkat cells, demonstrating an IC50 of 1.270 μM.

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.

β-Secretase Inhibitor III is a highly selective inhibitor of BACE1 with a Ki value of 0.13 nM.

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.

PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III) is a multikinase inhibitor that inhibits PDGFR, EGFR, FGFR, PKA, and PKC and can be used for research on amyotrophic lateral sclerosis [1].

FGFR1 inhibitor-9 (Compound 7) is a potent FGFR1 inhibitor with an IC50 of 0.85 nM, targeting the ATP-binding pocket of FGFR1 and demonstrating anticancer activity [1].

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

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].

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

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.

(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively).

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.

PDE-9 inhibitor is used for treatment neurodegenerative diseases.

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