AR-A014418

한글명:AR-A014418

카스 번호487021-52-3

상품명:AR-A014418

CBNumberCB9497883

분자식C12H12N4O4S

포뮬러 무게308.31

MOL 파일487021-52-3.mol

화학적 성질

녹는점	208-210?C (dec.)
밀도	1.464±0.06 g/cm3(Predicted)
저장 조건	2-8°C
용해도	DMSO: ≥20mg/mL, 투명, 연황색
물리적 상태	노란색 고체
산도 계수 (pKa)	5.80±0.70(Predicted)
색상	회백색부터 황갈색까지
감도	Light Sensitive
안정성	제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO의 솔루션은 -20°C에서 최대 2개월 동안 보관할 수 있습니다.

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

22-37/38-41

안전지침서

26-36/39

WGK 독일

NFPA 704:

	0
3		0

그림문자(GHS)

AR-A014418 화학적 특성, 용도, 생산

화학적 성질
Pale Yellow Solid
용도
AR-A014418 has been used as an inhibitor of glycogen synthase kinase 3 (GSK3).
일반 설명
A cell-permeable thiazole-containing urea compound that acts as a potent inhibitor of GSK-3. Shown to inhibit GSK-3β with high potency (IC₅₀ = 104 nM). Inhibition is competitive with respect to ATP (K_i = 38 nM). Specificity has been reported using a panel of 28 different kinases, including Cdk2 and Cdk5 (IC₅₀ >100 μM). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Aβ-mediated neurodegeneration in vitro and reduce tauopathy in mice in vivo (30 μmol/kg delivered with 40% PEG400 and 40% dimethylacetamide in water). Caution: Do not use delivering vehicles containing dimethylamine for in vivo studies, as it is highly toxic to animals. A 25 mM (5 mg/649 μl) solution of GSK-3β Inhibitor VIII (Cat. No. 361557) in DMSO is also available.
효소 저해제
This ATP-competitive protein kinase inhibitor (FW = 308.31 g/mol; CAS 487021-52-3; Solubility: 62 mg/mL DMSO; <1 mg/mL H2O) selectively targets glycogen synthase kinase 3β (GSK3β),with IC50 = 104 nM; Ki = 38 nM. Attesting to its high specificity for GSK3, AR-A014418 does not significantly inhibit Cdk2 or Cdk5 (IC50 > 100 μM) or 26 other kinases. AR-A014418 inhibits phosphorylation of the microtubule-associated protein Tau at Ser-396 (i.e., the GSK3-specific site) in cells stably expressing human four-repeat Tau. AR-A014418 protects N2A neuroblastoma cells against cell death mediated by inhibition of the phosphatidylinositol 3-kinase/protein kinase B survival pathway. AR- A014418 inhibits neurodegeneration mediated by b-amyloid peptide in hippocampal slices. Treatment of neuroblastoma cell lines with AR- A014418 reduced the level of GSK-3α phosphorylation at Tyr-279 compared to GSK-3β phosphorylation at Tyr-216, and attenuated growth via the maintenance of apoptosis.. AR-A014418-dependent antinociceptive effects are induced by modulation of the glutamatergic system through metabotropic and ionotropic (NMDA) receptors and the inhibition of TNF-α and IL-1β cytokine signaling.

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