Casein Kinase inhibitor A86是一种有效且具有口服活性的酪蛋白激酶 1α (CK1α) 抑制剂,同时也抑制 CDK7 (TFIIH) 和 CDK9 (P-TEFb),并能诱导白血病细胞凋亡 (apoptosis),具有抗白血病活性。
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产品名称 | PDGFR ↓ ↑ | PDGFRα ↓ ↑ | PDGFRβ ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tyrphostin A9 |
+
PDGFR, IC50: 0.5 μM |
EGFR | 98% | ||||||||||||||||
Tyrphostin AG1296 | 99%+ | ||||||||||||||||||
Motesanib Diphosphate |
++
PDGFR, IC50: 84 nM |
98% | |||||||||||||||||
Pazopanib |
++
PDGFR, IC50: 84 nM |
99% | |||||||||||||||||
Imatinib |
+
PDGFR, IC50: 100 nM |
c-Kit | 98% | ||||||||||||||||
Imatinib Mesylate |
+
PDGFR, IC50: 100 nM |
c-Kit | 99% | ||||||||||||||||
Sennoside B | ✔ | 99%+ | |||||||||||||||||
PP121 |
++++
PDGFR, IC50: 2 nM |
mTOR,VEGFR | 99%+ | ||||||||||||||||
Crenolanib |
++++
PDGFRα, Kd: 2.1 nM |
++++
PDGFRβ, Kd: 3.2 nM |
99%+ | ||||||||||||||||
Masitinib |
+
PDGFRα, IC50: 540 nM |
+
PDGFRβ, IC50: 800 nM |
99%+ | ||||||||||||||||
Ki8751 |
++
PDGFRα, IC50: 67 nM |
c-Kit | 98+% | ||||||||||||||||
Tivozanib |
++
PDGFRα, IC50: 40 nM |
++
PDGFRβ, IC50: 49 nM |
99%+ | ||||||||||||||||
Ponatinib |
++++
PDGFRα, IC50: 1.1 nM |
98% | |||||||||||||||||
Amuvatinib |
++
PDGFRα (V561D), IC50: 40 nM |
99%+ | |||||||||||||||||
Axitinib |
+++
PDGFRα, IC50: 5.0 nM |
++++
PDGFRβ, IC50: 1.6 nM |
98% | ||||||||||||||||
CP-673451 |
+++
PDGFRα, IC50: 10 nM |
++++
PDGFRβ, IC50: 1 nM |
99%+ | ||||||||||||||||
Telatinib |
+++
PDGFRα, IC50: 15 nM |
c-Kit | 99%+ | ||||||||||||||||
Nintedanib |
++
PDGFRα, IC50: 59 nM |
++
PDGFRβ, IC50: 65 nM |
99+% | ||||||||||||||||
Avapritinib |
++++
PDGFRα (D842V), IC50: 0.5 nM |
99%+ | |||||||||||||||||
MK-2461 |
+++
PDGFRβ, IC50: 22 nM |
98%+ | |||||||||||||||||
Lactate |
+++
PDGFRβ, IC50: 27 nM |
c-Kit,FLT3 | 85% | ||||||||||||||||
Linifanib |
++
PDGFRβ, IC50: 66 nM |
99%+ | |||||||||||||||||
AZD2932 |
+++
PDGFRβ, IC50: 4 nM |
c-Kit | 98% | ||||||||||||||||
Dovitinib |
+++
PDGFRβ, IC50: 27 nM |
c-Kit,FLT3 | 99%+ | ||||||||||||||||
Sorafenib |
++
mPDGFRβ, IC50: 57 nM PDGFRβ, IC50: 57 nM |
99% | |||||||||||||||||
Sunitinib |
++++
PDGFRβ , IC50: 2 nM |
FLT3 | 98% | ||||||||||||||||
Orantinib |
+++
PDGFRβ, Ki: 8 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。 |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.90mL 0.58mL 0.29mL |
14.52mL 2.90mL 1.45mL |
29.03mL 5.81mL 2.90mL |
CAS号 | 2079069-01-3 |
分子式 | C18H25FN6 |
分子量 | 344.43 |
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,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 12 mg/mL(34.84 mM),配合低频超声,并水浴加热至45℃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 |