Bentamapimod

SKU: orb1305180

Description

Bentamapimod (AS 602801) is an orally bioavailable, small-molecule inhibitor targeting the c-Jun N-terminal kinase (JNK) pathway. It is utilized in preclinical research to investigate JNK's role in cellular processes such as inflammation and apoptosis, with applications in both in vitro assays and in vivo disease models.

Research Area

Signal Transduction

Images & Validation

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Key Properties

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CAS Number	848344-36-5
MW	457.55
Purity	99.92% (May vary between batches)
Formula	C₂₅H₂₃N₅O₂S
SMILES	N#C\C(=C1\Nc2ccccc2S1)c1ccnc(OCc2ccc(CN3CCOCC3)cc2)n1
Target	JNK
Solubility	DMSO:4.58 mg/mL (10.01 mM)

Bioactivity

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Target IC50	JNK1:80 nM\|JNK2:90 nM\|JNK3:230 nM
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. Read more...
In Vitro	Bentamapimod treatment induces cell death and accordingly decreased the number of viable cells in all three cell lines in a dose-dependent manner, suggesting that Bentamapimod may have selective cytotoxic activity against neoplastic cells. Bentamapimod 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. Bentamapimod also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving Bentamapimod treatment. Read more...
Cell Research	AS 602801 (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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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AS 602801, AS602801, AS-602801, Bentamapimod, inhibit, JNK, JNK1, JNK2, JNK3, Inhibitor

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Compound Identifiers

PubChem CID

59427263 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	848344-36-5
MW:	457.55
Formula:	C₂₅H₂₃N₅O₂S

Bentamapimod

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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AS 602801 [orb1223036]

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