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Bentamapimod

Catalog No. T2675 CAS 848344-36-5

Synonyms: AS 602801

Bentamapimod (AS 602801) is a novel, orally active inhibitor of JNK.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Bentamapimod, CAS 848344-36-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 101.00
25 mg	In stock	$ 165.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
500 mg	In stock	$ 1,210.00
1 g	In stock	$ 2,190.00
2 g	In stock	$ 2,950.00

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Purity: 99.92%

Purity: 99.5%

Purity: 97.44%

Purity: 95.21%

Biological Description

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Storage & Solubility Information

Description	Bentamapimod (AS 602801) is a novel, orally active inhibitor of JNK.
Targets&IC50	JNK2:90 nM, JNK1:80 nM, JNK3:230 nM
In vitro	AS 602801 (AS602801) treatment induces cell death and accordingly decreased the number of viable cells in all three cell lines in a dose-dependent manner, suggesting that AS 602801 may have selective cytotoxic activity against neoplastic cells. 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[2].
In vivo	Treatment of nude mice bearing xenografts from women with endometriosis (BWE) with 30 mg/kg of AS 602801 (AS602801) resulted in a 29% reduction of lesions. In contrast, neither medroxyprogesterone acetate (MPA) nor progesterone (PR) alone led to regression of BWE lesions. However, a combination of 10 mg/kg AS 602801 with MPA achieved a 38% lesion regression. When applied to human endometrial organ cultures (from healthy women), AS 602801 or MPA decreased the release of matrix metalloproteinase-3 (MMP-3) into the culture medium. In BWE-established organ cultures, PR or MPA did not affect MMP-3 secretion, whereas AS 602801, either alone or in combination with MPA, effectively suppressed MMP-3 production. In an autologous rat endometriosis model, AS 602801 facilitated a 48% reduction in lesions, compared to an 84% reduction with the GnRH antagonist Antide. Additionally, AS 602801 diminished inflammatory cytokine levels in endometriotic lesions without altering cytokine levels in the ipsilateral horns. It also enhanced natural killer cell activity with no observed adverse effects on the uterus[3].
Cell Research	AS 602801 (AS602801) is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media before use[2]. 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[2].

Synonyms	AS 602801
Molecular Weight	457.55
Formula	C25H23N5O2S
CAS No.	848344-36-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.57 mg/mL (9.98 mM)

References and Literature

1. Messoussi A, et al. Recent progress in the design, study, and development of c-Jun N-terminal kinase inhibitors as anticanceragents. Chem Biol. 2014 Nov 20;21(11):1433-43. 2. Okada M, et al. The novel JNK inhibitor AS602801 inhibits cancer stem cells in vitro and in vivo. Oncotarget. 2016 May 10;7(19):27021-32. 3. Palmer SS, et al. Bentamapimod (JNK Inhibitor AS602801) Induces Regression of Endometriotic Lesions in Animal Models. Reprod Sci. 2016 Jan;23(1):11-23.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Prostate Cancer Compound Library Anti-Colorectal Cancer Compound Library Neural Regeneration Compound Library Anti-Ovarian Cancer Compound Library HIF-1 Signaling Pathway Compound Library

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Keywords

Bentamapimod 848344-36-5 MAPK JNK inhibit AS602801 Inhibitor AS 602801 AS-602801 inhibitor

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