aberrant

AZD-9574 is a selective inhibitor of PARP1 at the sites of SSBs. AZD-9574 exhibits anti-cancer activities and can be used in studies about HRD+ breast cancer and advanced solid malignancies.

Aberrant tau degrader 2 (Compound 4-12) acts as a degrader of tau protein and serves as a target protein ligand for the synthesis of PROTAC degrader C004019.

Aberrant tau ligand 1 serves as a binding agent for tau proteins in their abnormal configurations. It is utilized in the synthesis of the PROTAC aberrant Tau degrader, QC-01-175.

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

IACS-52825 is a selective and potent dual leucine zipper kinase (DLK) inhibitor that reverses para-mechanical aberrant pain in a CIPN mouse model for the study of neurological disorders.

h-NTPDase8-IN-1 is a specific aminosulfonylbenzamide inhibitor of h-NTPDases8 (IC 50 = 0.28 ± 0.07 μM). h-NTPDase8-IN-1 can be used to study diseases brought about by aberrant h -NTPDase expression.

3-Methoxytyramine (3-O-methyl Dopamine) is a cellular metabolite of dopamine (3-hydroxytyramine), a neuromodulator that induces behavioral effects, induces significant ERK and CREB phosphorylation, and is capable of inducing a complex set of aberrant involuntary movements in acutely depleted dopamine-containing mice.

Indibulin (D 24851) is a synthetic small molecule with antimitotic and potential antineoplastic activities.Indibulin an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.

Balamapimod, also known as MKI-822, is a small-molecule Ras/Raf/MEK inhibitor that directly targets deregulated MAPK signaling cascades and is being actively explored to suppress aberrant protein kinase activity implicated in oncogenic transformation, inflammatory signaling, and pathological cell proliferation, with demonstrated therapeutic relevance for stroke, osteoporosis, rheumatoid arthritis, polycystic kidney disease, colonic polyps, and other inflammation-driven disorders through pathway-level inhibition.

Rogaratinib (BAY1163877) is an aberrant inhibitor of fibroblast growth factor receptor (FGFR). Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity.

PB200, an HDAC6 inhibitor, demonstrates significant antidepressant effects with an IC50 value of 1.97 nM. It operates by normalizing aberrant HDAC6 expression levels and alleviating neuroinflammation.

PF-07265028 is an HPK1 inhibitor with an IC50 of 17 nM. Pharmacokinetic studies in mice and monkeys indicate that PF-07265028 exhibits moderate clearance, terminal half-life, volume of distribution, and oral bioavailability. It targets, binds, and inhibits Hpk1 activity, blocking Hpk1-mediated signaling pathways to prevent immune suppression mediated by Hpk1, including the inhibition of T-cell receptor (TCR) signaling, effector T-cell suppression, aberrant cytokine expression, and the elimination of the immunosuppressive tumor microenvironment (TME). This action can activate a cytotoxic T lymphocyte (CTL)-mediated immune response against tumor cells. Hpk1 is primarily expressed in hematopoietic cells and acts as a negative regulator of TCR signaling and T and B cell activation.

BR-cpd7 is a PROTAC degrader of fibroblast growth factor receptors (FGFR1/2) with a DC50 of 10 nM. It is capable of arresting the cell cycle and inhibiting the proliferation of tumor cells with aberrant activation of FGFR1/2.

QC-01-175 is a heterobifunctional small molecule specifically designed to induce degradation of aberrant tau protein, and it effectively reduces levels of A152T and P301L mutant tau, protects neurons from tau-mediated cytotoxicity. QC-01-175 significantly improves neuronal survival, thereby providing a valuable chemical biology tool for studying tauopathies and developing targeted protein degradation strategies for neurodegenerative diseases.

TNKS-2-IN-3 (Compound 5) is a selective and competitive inhibitor of Tankyrase 2 (TNKS2), with an IC50 value of 0.3 nM. It exhibits over 20-fold selectivity for TNKS2 compared to TNKS1 and more than 100-fold selectivity over PARP1/2. By inhibiting TNKS2-mediated ADP ribosylation, TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway, demonstrating antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 holds potential for research in solid tumors with aberrant Wnt pathway activation, such as colorectal cancer.

KBP-7018 is a potent and highly selective tyrosine kinase inhibitor that simultaneously targets three key fibrotic-associated kinases, including c-KIT, RET, and PDGFR, with IC50 values of 10 nM, 7.6 nM, and 25 nM respectively, and is therefore widely applicable for mechanistic research into fibrotic signaling pathways, kinase-driven disease progression, and pharmacological intervention strategies aimed at modulating aberrant tyrosine kinase activity.

2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid (3-Anthraniloylalanine) is a ketone and amino acid derivative with diverse biological functions, including vasodilatory, immunoregulatory, and neuromodulatory activities. It is a precursor for niacin and its aberrant production is linked to neurological disease-related cognitive deficits and depressive symptoms. This compound is overexpressed in certain cancer cell types and could potentially serve as a biomarker to assess cancer risk.

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.

BMS-984923 is an orally available and blood-brain barrier permeable mGluR5 silencing allosteric modulator that inhibits β-amyloid oligomer-induced aberrant synaptic signaling, and can be used to study Alzheimer's disease.

Tilpisertib is a serine/threonine kinase inhibitor disclosed in patent WO2017007689, designed to modulate aberrant kinase-driven signaling pathways, and is used extensively in cancer biology and signal transduction research to investigate kinase-dependent cell proliferation, survival, and resistance mechanisms, supporting preclinical evaluation of targeted therapeutic strategies.

SSE15206 is a microtubule polymerization inhibitor that overcomes multidrug resistance, causing aberrant mitosis and resulting in G2/M arrest due to incomplete spindle formation in cancer cells.

cis-4-Br-2,5-F2-PCPA (S1024) inhibits LSD1 and LSD2 with Ki values of 94 nM and 8.4 μM, respectively. It inhibits LSD1 cell proliferation and increases dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells, particularly where there is aberrant expression of LSD1 in cancer stem cells [1].

LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1) with a Ki value of 11 nM, compared to 7 μM for LSD2. Aberrant expression of LSD1 is found in tumor stem cells, and LSD1/2-IN-1 inhibits LSD1 cell proliferation [1].

(S)-Cdc7-IN-18, a potent CDC7 inhibitor, effectively impedes the overactivation of MCM2, a crucial tumor cell marker, induced by huCdc7 overexpression. Consequently, it inhibits the aberrant proliferation of tumor cells. This compound, exhibits promise for cancer disease research [1].