TAK-715 | p38 MAPK Inhibitor | AmBeed-信号通路专用抑制剂

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TAK-715 {[allProObj[0].p_purity_real_show]}

货号：A302845

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, being 28-fold selective for p38α over p38β, showing no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.

TAK-715 化学结构
CAS号：303162-79-0

TAK-715 3D分子结构
CAS号：303162-79-0

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TAK-715 纯度/质量文件产品仅供科研

货号：A302845 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

p38 MAPK 亚型比较
Casein Kinase 亚型比较

产品名称	p38 MAPK ↓ ↑	p38α ↓ ↑	p38β ↓ ↑	其他靶点	纯度
BMS-582949	+++ p38 MAPK, IC50: 13 nM				98%
SB 203580					99%+
Pexmetinib	✔			Tie-2	99%+
Skepinone-L		++++ p38α, IC50: 5 nM			98%
Doramapimod		++++ p38α, Kd: 0.1 nM p38α, IC50: 38 nM			99%+
VX-702					99%+
Ralimetinib dimesylate		++++ p38α, IC50: 7 nM			98%
SB 202190		++ p38α, IC50: 50 nM	++ p38β, IC50: 100 nM		99%+
Losmapimod		++++ p38α, pKi: 8.1	+++ p38β, pKi: 7.6		99%+
Neflamapimod		+++ p38α, IC50: 10 nM	+ p38β, IC50: 220 nM		99%+
PH-797804		++ p38α, IC50: 26 nM	+ p38β, IC50: 102 nM		98%
TAK-715		++++ p38α, IC50: 7.1 nM	+ p38β, IC50: 0.20 μM		99%+
SB 239063		++ p38α, IC50: 44 nM	++ p38β, IC50: 44 nM		99%+
Pamapimod		+++ p38α, IC50: 0.014 μM	+ p38β, IC50: 0.48 μM		98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	CK1 ↓ ↑	CK2 ↓ ↑	其他靶点	纯度
PF-670462 2HCl	++++ CK1ε, IC50: 90 nM CK1δ, IC50: 13 nM			99%+
D4476	++ CK1 from Schizosaccharomyces pombe, IC50: 200 nM CK1δ, IC50: 300 nM			98%
SR-3029	+++ CK1ε, IC50: 260 nM CK1δ, IC50: 44 nM			99%+
IWP-2	+++ ^M82FCK1δ, IC50: 40 nM		Wnt	98%
LY364947	++ CK1δ, IC50: 0.22 μM			98%
TA-01	++++ CK1ε, IC50: 6.4 nM CK1δ, IC50: 6.8 nM		p38 MAPK	99%+
IC261	+ CK1, IC50: 16 μM			98%
PF-4800567	+++ casein kinase 1 delta, IC50: 711 nM casein kinase 1 epsilon, IC50: 32 nM			99%+
CK1-IN-1	++++ CK1ε, IC50: 16 nM CK1δ, IC50: 15 nM			98%
Longdaysin	+ CKIα, IC50: 5.6 μM CKIδ, IC50: 8.8 μM			99%+
Silmitasertib		++++ CK2, IC50: 1 nM		99%+
Ellagic acid (hydrate)		+++ CK2, IC50: 0.04 μM	PKA	95+%
DMAT		+++ CK2, Ki: ~40 nM		98%
Hematein		++ CK2, IC50: 0.55 μM		98+%
Silmitasertib sodium salt		++++ CK2α, IC50: 1 nM CK2α', IC50: 1 nM		99%+
LY294002		+++ CK2, IC50: 98 nM		99%+
A-3 HCl	+ CK1, Ki: 80 μM	++ CK2, Ki: 5.1 μM	MLCK,PKA,PKC	98+%
TBB	+ CK1, Ki: 47 μM	++ CK2, Ki: 0.4 μM		98%
TTP 22		++ CK2, IC50: 100 nM		98%+
DRB		✔		99%+
BioE-1115		+ CK2α, IC50: 10 μM		99%+
(E/Z)-GO289		++++ CK2, IC50: 7 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

TAK-715 生物活性

靶点	p38β p38β, IC50:0.20 μM p38α p38α, IC50:7.1 nM
描述	The stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. The well reported isoforms of p38 MAPKs include p38α, p38β and others. TAK-715 is a p38 MAPK inhibitor, with selectivity for p38α. The inhibitory IC₅₀ of TAK-715 against p38α was 7.1nM while the data against p38β was 200nM. TAK-715 was not active against p38γ, p38δ, or other kinases. TAK-715 inhibited LPS-stimulated release of TNFα from THP-1 cells with an IC₅₀ of 48 nM^[3]. At the concentration of 10μM, TAK-715 inhibited Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells^[4]. Orally administrated at the dose of 10mg/kg, TAK-715 resulted in 87.6% inhibition of LPS-induced TNFα production in mice. In an adjuvant-induced arthritis model in rats, TAK-715 dose dependently inhibited paw swelling when given daily for 14 days at 3mg/kg, 10mg/kg or 30mg/kg^[3].
作用机制	TAK-715 target p38α in an ATP-competitive manner^[4].

TAK-715 参考文献

[1]Verkaar F, van der Doelen AA, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94.

[2]Miwatashi S, Arikawa Y, et al. Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl] -2-pyridyl] benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem. 2005 Sep 22;48(19):5966-79.

[3]Miwatashi S, Arikawa Y, Kotani E, Miyamoto M, Naruo K, Kimura H, Tanaka T, Asahi S, Ohkawa S. Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem. 2005 Sep 22;48(19):5966-79.

[4]Verkaar F, van der Doelen AA, Smits JF, Blankesteijn WM, Zaman GJ. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94.

TAK-715 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.03mL

5.01mL

2.50mL

TAK-715 技术信息

CAS号	303162-79-0
分子式	C₂₄H₂₁N₃OS
分子量	399.508

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(262.82 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

30% propylene glycol+5% Tween 80+65% water 30 mg/mL suspension

TAK-715 {[allProObj[0].p_purity_real_show]}

TAK-715 纯度/质量文件产品仅供科研

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TAK-715 {[allProObj[0].p_purity_real_show]}

TAK-715 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

TAK-715 质控信息

TAK-715 生物活性

TAK-715 参考文献

TAK-715 实验方案

TAK-715 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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TAK-715 纯度/质量文件产品仅供科研