adp-ribosylation

QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor. Modulates ARF-GTP levels and synergizes with the Wnt/β-catenin signaling pathway to upregulate β-catenin nuclear translocation. Also reduces in vitro migration of metastatic human breast cancer cells.

TIQ-A is a PARP1 inhibitor which involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is triggered by DNA damage and its excessive activation has been proposed as a causative factor in many pathological conditions includi

Iobenguane sulfate (MIBG sulfate) is a high-affinity substrate for cholera toxin that disrupts cellular mono(ADP-ribosylation). Radioiodinated Iobenguane sulfate is used clinically as a tumor-targeted radiopharmaceutical for diagnosing and treating adrenergic tumors.

K-756 is a direct and selective inhibitor of tankyrase (TNKS), inhibiting the ADP-ribosylation activity of TNKS1 [IC50 = 31 nM] and TNKS2 [IC50 = 36 nM].

G-631 acts as a selective tankyrase inhibitor, effectively hindering tankyrase auto-PARsylation (poly ADP ribosylation) at an IC 50 of 7 nM and suppressing the Wnt signaling pathway. This compound also demonstrates favorable pharmacokinetic properties in mice.

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.

Arf1-GEFs-IN-1 is a potent and orally active inhibitor of ADP-ribosylation factor 1-guanine nucleotide exchange factors (Arf1-GEFs), exhibiting an IC50 value of 40 μM in CT26 cells. Primarily, Arf1-GEFs-IN-1 induces tumor regression by triggering anti-tumor immune responses rather than direct cytotoxicity. It effectively enhances CCL5 expression and demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 is applicable in colon cancer research.

Guanylyl Imidodiphosphate trisodium (Guanosine 5'-[β,γ-imido]triphosphate), a non-hydrolysable GTP analogue, activates ADP-ribosylation factor (ARF) and strongly stimulates adenylate cyclase. It is utilized in protein synthesis studies [1] [2] [3].

CHS-111 is a benzyl indazole compound that inhibits superoxide anion (O(2)(-)) generation and reduces fMLP-stimulated PLD activity (IC(50) 3.9±1.2μM). It inhibits the interaction of PLD1 with ADP-ribosylation factor (Arf) 6 and Ras homology (Rho) A, and reduces the membrane recruitment of RhoA in fMLP-stimulated cells.

Glutamyl ribose 5-phosphate is obtained by the linkage region in ADP ribosylation of proteins.

Fluoroscein NAD+ is a substrate for ADP-ribosylation, providing a convenient non-isotopic alternative to radiolabelled NAD for use in PARP assays. Allows direct measurement of NAD-dependent enzymes, such as PARP, by fluorescence microscopy. This product is a replacement for R&D Systems product 4673-500-01 81 μg is supplied as 250 μl of a 0.25 mM solution in water.

cis-Resveratrol ((Z)-Resveratrol) has antiviral activity, inhibits enteroviruses, increases TyrRS, promotes histone serine-ADP ribosylation-dependent DNA repair, and provides neuroprotection in a TyrRS-dependent manner.

AV-153 is a 1,4-dihydropyridine derivative with antimutagenic properties. It intercalates into DNA at single strand breaks, resulting in reduced DNA damage and stimulation of DNA repair in human cells in vitro. AV-153 also interacts with thymine and cytosine and influences poly(ADP)ribosylation. Moreover, AV-153 exhibits anti-cancer activity.

AV-153 free base is a 1,4-dihydropyridine (1,4-DHP) derivative with antimutagenic and anti-cancer activity. It interacts with cytosine and thymine, influences poly(ADP)ribosylation, intercalates to DNA at single-strand breaks, reduces DNA damage, and stimulates DNA repair in human cells in vitro [1] [2] [3].

RBN-3143 is a potent inhibitor of NAD+-competitive catalytic PARP14 (IC50= 4 nM), which inhibits ADP-ribosylation mediated by PARP14 and stabilizes PARP14 in cell lines, demonstrating research potential for lung inflammation.

M-COPA is a golgi disruptor which inhibits cell surface expression of MET protein and the ADP-ribosylation factor 1 (Arf1) activation. M-COPA also inhibits angiogenesis through suppression of both VEGFR1/2 and nuclear factor-kappaB (NF-kappaB) signaling pathways.

MC2050 is a potent PARP-1 inhibitor. The IC50 for inhibition of PARP-1 activity is 119 nM, compared to 1.8 μM for PARP-2. MC2050 inhibits apoptosis and blocks poly ADP-ribosylation of histone H1 in hydrogen peroxide treated SH-SY5Y neuroblastoma cells.

β-Nicotinamide adenine dinucleotide reduced dipotassium is an orally active, reduced coenzyme that functions as a donor of ADP-ribose units in ADP-ribosylation reactions and as a precursor of cyclic ADP-ribose. It also serves as a regenerative electron donor in essential cellular energy metabolism processes, including glycolysis, β-oxidation, and the tricarboxylic acid (TCA) cycle [1].

Nicotinamide 1,N6-ethenoadenine dinucleotide (ε-NAD) is a fluorescent analog of NAD that serves as a fluorescent substrate for studying ADP-ribosylation reactions.

1-Palmitoyl-2-stearoyl-rac-glycerol, a diacylglycerol, features palmitic acid at the sn-1 position and stearic acid at the sn-2 position. This compound plays a role in identifying the fatty acyl chain properties of diacylglycerols that activate the ADP-ribosylation factor 1 GTPase-activating protein (ARF1 GAP).

NADH disodium salt hydrate, also known as Disodium NADH hydrate, functions as an orally active reduced coenzyme. It serves as a donor of ADP-ribose units in ADP-ribosylation reactions and acts as a precursor to cyclic ADP-ribose. Additionally, it contributes to cellular energy metabolism by acting as a renewable electron donor in processes such as glycolysis, β-oxidation, and the tricarboxylic acid (TCA) cycle [1].

ARF (26–44) acetate (935732-44-8 free base) is a polypeptide fragment derived from the C-terminal of ADP ribosylation factor (ARF) protein, which is often used to study vesicle transport and membrane dynamics related to ARF. The peptide can interact with ARF effector protein or membrane structure in vitro, and is widely used as a tool molecule to analyze the mechanism of ARF-mediated signal transduction and intracellular membrane transport.

Nicotinamide 1,N6-ethenoadenine dinucleotide (ε-NAD) sodium is a fluorescent analog of NAD, serving as a substrate for bacterial toxins that catalyze the G-ADP ribosylation of signal-transduction G proteins. Additionally, Nicotinamide 1,N6-ethenoadenine dinucleotide sodium can be used as a fluorescent substrate in the study of ADP ribosylation reactions.

Fluorescein-NAD+ sodium serves as an alternative to radiolabeled NAD and acts as a substrate for ADP-ribosylation. It is applicable in PARP assays and has an extinction coefficient of 262 nm.