AS601245 (Synonyms: AS-601245, c-Jun N-terminal Kinase Inhibitor V) |
رقم الكتالوجGC10010
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AS601245 هو مثبط JNK نشط عن طريق الفم ، انتقائي ، ATP تنافسي (c-Jun NH2- بروتين كيناز) مع IC50s من 150 ، 220 ، و 70 نانومتر لثلاثة أشكال إسوية بشرية JNK (hJNK1 ، hJNK2 ، و hJNK3) ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 345987-15-7
Sample solution is provided at 25 µL, 10mM.
AS601245 is a potent ATP-competitive JNK inhibitor with IC50 values of 0.15µM, 0.22, and 0.07µM for JNK1, JNK2, and JNK3, respectively [1]. AS601245 can prevent P-TEFb from being released from the inactive complex formed with HEXIM-1, and interfere with the reactivation of the HIV-1 virus at multiple levels[2]. AS601245 has been widely used to inhibit the growth of follicular cells and interfere with the progression of the cell cycle[3].
In vitro, AS601245 treatment for 96h significantly inhibited the proliferation of CaCo-2 cells, with an IC50 value of 2.5µM[4]. 0.1µM of AS601245 treatment for 24 hours significantly increased the expression of p21 in HepG2 cells and inhibited cell viability[5]. Treatment with 10µM AS601245 for 24 hours significantly promoted apoptosis of SH-SY5Y cells, accompanied by an increase in caspase-3 activity, expression of pro-apoptotic proteins, as well as significant disruptions in oxidative phosphorylation and glycolysis[6].
In vivo, AS601245 treatment via intraperitoneal injection at a dose of 80mg/kg at 15 minutes and 24 hours after restoration of carotid artery flow prevented neurite loss, reduced astrogliosis, and improved long-term memory deficits induced by cerebral ischemia in gerbils [7]. A single oral administration of 10mg/kg dose of AS601245 significantly inhibited the release of TNF-α in mice caused by endotoxins[8].
References:
[1] Malemud C J. Small molecular weight inhibitors of stress-activated and mitogen-activated protein kinases[J]. Mini Reviews in Medicinal Chemistry, 2006, 6(6): 689-698.
[2] Wolschendorf F, Bosque A, Shishido T, et al. Kinase control prevents HIV-1 reactivation in spite of high levels of induced NF-κB activity[J]. Journal of virology, 2012, 86(8): 4548-4558.
[3] Oktem O, Oktay K. c-Jun N-terminal kinase (JNK) pathway controls granulosa cell mitosis: a novel mechanism in regulation of preantral follicle growth[J]. Fertility and Sterility, 2008, 90: S330.
[4] Cerbone A, Toaldo C, Minelli R, et al. Rosiglitazone and AS601245 decrease cell adhesion and migration through modulation of specific gene expression in human colon cancer cells[J]. PLoS One, 2012, 7(6): e40149.
[5] Cerbone A, Toaldo C, Pizzimenti S, et al. AS601245, an anti‐inflammatory JNK inhibitor, and Clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo‐2 colon cancer cells[J]. PPAR research, 2012, 2012(1): 269751.
[6] Granek Z, Siwecka N, Saramowicz K, et al. Pharmacological Inhibition of JNK Signalling Exerts Anti-Neoplastic Effects on SH-SY5Y Human Neuroblastoma Cells[J]. International Journal of Molecular Sciences, 2025, 26(24): 11894.
[7] Carboni S, Boschert U, Gaillard P, et al. AS601245, ac‐Jun NH2‐terminal kinase (JNK) inhibitor, reduces axon/dendrite damage and cognitive deficits after global cerebral ischaemia in gerbils[J]. British journal of pharmacology, 2008, 153(1): 157-163.
[8] Carboni S, Hiver A, Szyndralewiez C, et al. AS601245 (1, 3-Benzothiazol-2-yl (2-{[2-(3-pyridinyl) ethyl] amino}-4 pyrimidinyl) Acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties[J]. The Journal of pharmacology and experimental therapeutics, 2004, 310(1): 25-32.
| Cell experiment [1]: | |
Cell lines | CaCo-2 cells |
Preparation Method | CaCo-2 cells were grown in DMEM medium with 10% (v/v) fetal bovine serum (FBS), 2 mM glutamine, 1% non-essential amino acids solution, and 1% antibiotic mixture (penicillin-streptomycin) at 37°C in 5% CO2/atmosphere. CaCo-2 cells (3×103 cells) were seeded in 96-well plates, incubated for 24h, and then treated with different concentrations of AS601245 (0.1, 1, 10, and 50µM) at 37°C. After 96h, cell viability was measured. |
Reaction Conditions | 0.1, 1, 10, and 50µM; 96h |
Applications | AS601245 treatment significantly reduced the cell viability of CaCo-2 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | C3H/HEN mice |
Preparation Method | C3H/HEN mice were kept in a temperature-controlled (20-22°C) and light/dark cycle-controlled animal room (lights on at 7:00 AM and off at 7:00 PM). Standard laboratory chow and water were available ad libitum. Mice received an oral treatment with AS601245 (10mg/kg in 0.5% CMC/0.25% Tween 20). Fifteen minutes later, endotoxins (O111:B4; 0.3mg/kg) were i.p. injected. Heparinized whole blood was collected by retroorbital puncture under isoflurane anesthesia. TNF-α was determined in plasma. |
Dosage form | 10mg/kg for once; p.o. |
Applications | AS601245 treatment significantly reduced TNF-α levels in mice after treatment with endotoxins. |
References: | |
| Cas No. | 345987-15-7 | SDF | |
| المرادفات | AS-601245, c-Jun N-terminal Kinase Inhibitor V | ||
| Chemical Name | (Z)-2-(benzo[d]thiazol-2-yl)-2-(2-((2-(pyridin-3-yl)ethyl)imino)-1,2-dihydropyrimidin-4-yl)acetonitrile | ||
| Canonical SMILES | N#CC(C1=NC2=CC=CC=C2S1)C(C=CN/3)=NC3=N/CCC4=CN=CC=C4 | ||
| Formula | C20H16N6S | M.Wt | 372.45 |
| الذوبان | ≥ 14.25mg/mL in DMSO, ≥ 10mg/mL in Water with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6849 mL | 13.4246 mL | 26.8492 mL |
| 5 mM | 537 μL | 2.6849 mL | 5.3698 mL |
| 10 mM | 268.5 μL | 1.3425 mL | 2.6849 mL |
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)