货号:A662677 产品仅供科研
SR-3029 is a potent and highly specific CK1δ/CK1ε inhibitor with the IC50 of 97 nM.
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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 |
99%+ | |||||||||||||||||
PF-4800567 |
+++
casein kinase 1 epsilon, IC50: 32 nM casein kinase 1 delta, IC50: 711 nM |
99%+ | |||||||||||||||||
CK1-IN-1 |
++++
CK1ε, IC50: 16 nM CK1δ, IC50: 15 nM |
98% | |||||||||||||||||
Longdaysin |
+
CKIδ, IC50: 8.8 μM CKIα, IC50: 5.6 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,PKC,PKA | 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 |
98%+ | |||||||||||||||||
(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。 |
靶点 |
|
描述 | SR-3029 is a strong inhibitor of CK1δ/CK1ε, with IC50 values of 44 nM and 260 nM, respectively. It competes with ATP, having Kis of 97 nM for CK1δ/CK1ε. SR-3029 also inhibits CDK6/cyclin D3, CDK6/cyclin D1, CDK4/cyclin D3, CDK4/cyclin D1, and FLT3, with IC50s of 427, 428, 368, 576, and 3000 nM, respectively. It exhibits inhibitory activity on A375 cells, with an EC50 of 86 nM[1]. SR-3029's efficacy is lower against MCF7 and T47D breast cancer cells, as well as the MCF10A cell line, all of which have low CK1δ expression[2]. |
Animal study | Administered at 20 mg/kg daily via intraperitoneal injection, SR-3029 shows anti-tumor properties in orthotopic MDA-MB-231, MDA-MB-468 (TNBC), SKBR3, and BT474 (HER2+) tumor xenografts without apparent toxicity in mice. The same dosage of SR-3029 also effectively suppresses tumor growth in primary patient-derived xenograft (PDX) models and significantly lowers nuclear β-catenin expression in the tumors of treated mice[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.08mL 0.42mL 0.21mL |
10.41mL 2.08mL 1.04mL |
20.81mL 4.16mL 2.08mL |
CAS号 | 1454585-06-8 |
分子式 | C23H19F3N8O |
分子量 | 480.445 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 30 mg/mL(62.44 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 |