All AbMole products are for research use only, cannot be used for human consumption.
Bentamapimod, also known as AS602801, is an ATP-competitive JNK inhibitor with IC50 of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively. AS 602801 exhibits cytotoxicity against both serum-cultured non-stem cancer cells and cancer stem cells derived from human pancreatic cancer, non-small cell lung cancer, ovarian cancer and glioblastoma at concentrations that did not decrease the viability of normal human fibroblasts. AS 602801 also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving AS 602801 treatment.
In vivo: Bentamapimod (30 mg/kg) on nude mice bearing xenografts biopsied from women with endometriosis (BWE) causes 29% regression of lesion. In human endometrial organ cultures (from healthy women), treatment with AS-602801 or MPA reduced matrix metalloproteinase-3 (MMP-3) release into culture medium. In organ cultures established with BWE, PR or MPA failed to inhibit MMP-3 secretion, whereas AS 602801 alone or MPA + AS 602801 suppresses MMP-3 production. In an autologous rat endometriosis model, AS 602801 causes 48% regression of lesions compared to GnRH antagonist Antide (84%). Bentamapimod reduces inflammatory cytokines in endometriotic lesions, while levels of cytokines in ipsilateral horns are unaffected.
| Cell Experiment | |
|---|---|
| Cell lines | PANC-1, A2780, and A549 human cancer cells |
| Preparation method | Bentamapimod (AS602801) is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media before use. PANC-1, A2780, and A549 human cancer cells and IMR90 human normal fibroblasts are treated without (control) or with the indicated concentrations of AS 602801 (2.5, 5, and 7.5 μM) for 3 days. The number of viable cells (left panels) and the percentage of dead cells (right panels) are determined using trypan blue as a vital dye. |
| Concentrations | 2.5, 5, and 7.5 μM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | 5-week-old athymic (ncr/nude) ovariectomized mice |
| Formulation | dissolved in in DMSO (10 mM) and diluted with PBS |
| Dosages | 10 mg/kg and 30 mg/kg/animal for 30 days |
| Administration | gavage |
| Molecular Weight | 457.55 |
| Formula | C25H23N5O2S |
| CAS Number | 848344-36-5 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related JNK Products |
|---|
| JNK-IN-8
JNK-IN-8 (JNK Inhibitor XVI) is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively. |
| SP600125
SP600125 is a novel and selective inhibitor of c-Jun N-terminal kinase (JNK), inhibited phosphorylation of c-Jun with an IC50 of 5-10 microM. |
| JNK Inhibitor IX
JNK inhibitor IX is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively. |
| Cinobufagin
Cinobufagin is a cardiotoxic bufanolide steroid secreted by the Asiatic toad Bufo gargarizans. |
| Polyphyllin-I
Polyphyllin I is a bioactive ingredient extracted from Paris Polyphylla with strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
