aberrant

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.

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.

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.

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.

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 a highly potent and selective small-molecule inhibitor of hematopoietic progenitor cell kinase 1 (HPK1/MAP4K1). By blocking HPK1-mediated signal transduction, PF-07265028 enhances T-cell receptor-associated signaling, thereby lifting immune suppression and promoting antitumor immune responses. PF-07265028 exhibits significant activity at the cellular level (e.g., inhibition of pSLP76, IC₅₀ approximately 17 nM). PF-07265028 is suitable for use in cancer research.

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.

MYC-IN-4 is a MYC inhibitor that disrupts the interaction between MYC/MAX proteins with an IC50 of 3.06 μM. It inhibits MYC-aberrant PC-3 prostate cancer cells, exhibiting an IC50 of 0.440 μM. In FVB mice with Myc-CaP prostate tumor xenografts, MYC-IN-4 demonstrates significant antitumor efficacy. This compound is useful for prostate cancer research.

BRM/BRG1 ATP-IN-8 (Compound Cpd14) is an orally effective inhibitor of the BRG1/BRM enzyme domain. It exerts antitumor effects by disrupting aberrant chromatin remodeling in cancer cells, inducing apoptosis, and causing growth arrest. This compound is promising for research on BRG1/BRM-dependent malignancies, including hematologic cancers, prostate cancer, breast cancer, and Ewing's sarcoma.

STAT3-IN-52 (Compound 9) is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3). It binds to the pY705 site of STAT3 with a Ki of 440 nM, effectively hindering STAT3 phosphorylation and dimerization. STAT3-IN-52 exhibits potent cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 of 0.7 μM), medulloblastoma UW426, and pancreatic cancer BKPC3 cells. The compound induces apoptosis, inhibits STAT3's nuclear translocation and DNA-binding activity, and downregulates the expression of the STAT3 target gene MMP9. STAT3-IN-52 is useful in research related to cancers with aberrant STAT3 activation.

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.