In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
A-966492 is an inhibitor of PARP-1 with Ki value of 1nM .
PARP-1 belongs to the poly(ADP-ribose) polymerases (PARPs) family, it contributes to the resistance happened after cancer therapy. A-966492 is a potent inhibitor of both PARP-1 and PARP-2 (Ki value of 1.5nM) with good potency in C41 whole cells (EC50 value of 1nM). A-966492 shows excellent pharmaceutical properties with oral bioavailabilities of 34-72% and half-lives of 1.7-1.9 h. Additionally, A-966492 can crosses the blood-brain barrier. A-966492 is proved potent in a murine B16F10 syngeneic melanoma model and a BRCA1-deficient MX-1 breast carcinoma model. Meanwhile, it can enhance the efficacy of TMZ and carboplatin in these models .
 Penning TD, Zhu GD, Gong J, Thomas S, Gandhi VB, Liu X, Shi Y, Klinghofer V, Johnson EF, Park CH, Fry EH, Donawho CK, Frost DJ, Buchanan FG, Bukofzer GT, Rodriguez LE, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL. Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor. J Med Chem. 2010 Apr 22;53(8):3142-53.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥32.4 mg/mL in DMSO, ≥3.16 mg/mL in EtOH with ultrasonic and warming, ≥16.53 mg/mL in H2O with ultrasonic|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.|
|IC50||1 nM||1.5 nM|