Longdaysin | CK1 Inhibitor | AmBeed-信号通路专用抑制剂

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Longdaysin {[allProObj[0].p_purity_real_show]}

货号：A1177302

Longdaysin inhibited CKIδ, CKIα, ERK2 and CDK7 with IC50 values of 8.8, 5.6, 52, and 29μM, respectively. The EC50 values of longdaysin for CKIδ and CKIα in the cell-based PER1 degradation assay were 9.7 and 9.2μM, respectively.

Longdaysin 化学结构
CAS号：1353867-91-0

Longdaysin 3D分子结构
CAS号：1353867-91-0

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Longdaysin 纯度/质量文件产品仅供科研

货号：A1177302 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 >

ERK 亚型比较
CDK 亚型比较
Casein Kinase 亚型比较

产品名称	ERK ↓ ↑	ERK1 ↓ ↑	ERK2 ↓ ↑	ERK5 ↓ ↑	其他靶点	纯度
DEL-22379	+ ERK, IC50: 0.5 μM			+ ERK, IC50: 0.5 μM		98%
Pluripotin		++ ERK1, Kd: 98 nM			RasGAP	98+%
FR 180204		+ ERK1, Ki: 0.31 μM	++ ERK2, Ki: 0.14 μM			98%
Ravoxertinib		+++ ERK1, IC50: 1.1 nM	++++ ERK2, IC50: 0.3 nM			99%+
SCH772984		+++ ERK1, IC50: 4 nM	++++ ERK2, IC50: 1 nM			99%+
Temuterkib		+++ ERK1, IC50: 5 nM	+++ ERK2, IC50: 5 nM			99%+
VX-11e			+++ ERK2, Ki: <2 nM			99%+
Ulixertinib			++++ ERK2, IC50: <0.3 nM			99%+
XMD17-109				++ ERK5, IC50: 162 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。

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											ERK,SGK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	98%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	98%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				98+%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 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。

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。

Longdaysin 生物活性

靶点

CK1

CKIα, IC50:5.6 μM

CKIδ, IC50:8.8 μM

描述

The casein kinase I (CKI) family is a group of serine/threonine-selective enzymes that function as regulators of signaling pathways involved in circadian rhythms, DNA repair and Wnt signaling. As measured in the in vitro kinase assay, longdaysin inhibited CKIδ, CKIα, ERK2 and CDK7 with IC50 values of 8.8, 5.6, 52, and 29μM, respectively. The EC50 values of longdaysin for CKIδ and CKIα in the cell-based PER1 degradation assay were 9.7 and 9.2μM, respectively. Treatment with longdaysin (0–9μM) led to dose-dependent period lengthening in adult tail fibroblasts, lung explants, and suprachiasmatic nucleus explants from mPer2^Luc knockin mice. Longdaysin at the doses of 0.01–9μM also lengthened the period in both wild-type and CKIδ-deficient embryonic fibroblasts in a dose-dependent manner. In HEK293T cells, 10μM longdaysin reduced the CKIδ- and CKIα-dependent mobility-shift of PER1. The CKIδ- and CKIα-dependent degradation of PER1 was dose-dependently inhibited by longdaysin at the concentrations of 0-20μM. Moreover, longdaysin treatment (3 and 9µM) greatly upregulated the overall protein amount of PER1 in Bmal1-dLuc U2OS cells when compared to non-longdaysin treated controls. The administration of longdaysin (0–9μM) also resulted in >10h period lengthening in per3-luc reporter zebrafish in a dose-dependent manner^[1].

Longdaysin 动物研究

Dose	Mice: 5 mg/kg^[1] (i.p.)
Administration	i.p.

Longdaysin 参考文献

[1]Hirota T, Lee JW, Lewis WG, Zhang EE, Breton G, Liu X, Garcia M, Peters EC, Etchegaray JP, Traver D, Schultz PG, Kay SA. High-throughput chemical screen identifies a novel potent modulator of cellular circadian rhythms and reveals CKIα as a clock regulatory kinase. PLoS Biol. 2010 Dec 14;8(12):e1000559.

Longdaysin 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.98mL

0.60mL

0.30mL

14.91mL

2.98mL

1.49mL

29.82mL

5.96mL

2.98mL

Longdaysin 技术信息

CAS号	1353867-91-0
分子式	C₁₆H₁₆F₃N₅
分子量	335.327

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 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 120 mg/mL(357.86 mM)，配合低频超声助溶，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

Longdaysin {[allProObj[0].p_purity_real_show]}

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Longdaysin 动物研究

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最近浏览的产品

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摩尔计算器

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总药量计算器

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