货号:A899287 同义名: (R)-CR8;CR8, (R)-Isomer
(R)-CR8 is a cyclin dependent kinase (cdk) inhibitor with IC50 of 0.036 - 0.07 and 0.09 - 0.8 μM for cdk2 and cdk1,respectively.
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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/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM |
+
CDK4/CyclinD1, IC50: 850 nM |
99%+ | |||||||||||||||
SCH900776 |
++
CDK2, IC50: 0.16 μM |
99%+ | |||||||||||||||||
AUZ 454 |
++++
CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM |
99%+ | |||||||||||||||||
A-674563 HCl |
++
CDK2, Ki: 46 nM |
PKA | 98% | ||||||||||||||||
JNJ-7706621 |
++++
CDK1/CyclinB, IC50: 9 nM |
++++
CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 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/CyclinA, IC50: 8 nM CDK2/CyclinE, 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/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM |
++
CDK4/CyclinD1, IC50: 160 nM |
+
CDK5/p35, IC50: 265 nM |
++
CDK7/CyclinH, IC50: 150 nM |
99%+ | |||||||||||||
Kenpaullone |
+
CDK1/CyclinB, IC50: 0.4μM |
+
CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM |
+
CDK5/p35, IC50: 0.85μM |
98% | |||||||||||||||
SNS-032 |
+++
CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 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/CyclinA, IC50: 0.7 μM CDK2/CyclinE, 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/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 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/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 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/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM |
++
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。 |
描述 | Cyclin-dependent kinases (Cdks) are serine/threonine kinases and their catalytic activities are modulated by interactions with cyclins and Cdk inhibitors (CKIs)[1]. (R)-CR8 inhibits CDK1/cyclin B (IC50=0. 09 μM), CDK2/cyclin A (0. 072 μM), CDK2/cyclin E (0. 041 μM), CDK5/p25 (0. 11 μM), CDK7/cyclin H (1. 1 μM), CDK9/cyclin T (0. 18 μM) and CK1δ/ε (0. 4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect[2]. (R)-CR8 (5 mg/Kg; i. p. ) results in a significant reduction in lesion size at 28 days in histological assessment[3]. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K. The CDK-bound form of (R)-CR8 has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradation[4]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01659437 | Mycobacterium Ulcerans Infecti... 展开 >>on 收起 << | Phase 2 Phase 3 | Active, not recruiting | January 2018 | Benin ... 展开 >> Pobè Treatment Center Pobè, Benin Ghana Agogo Presbyterian Hospital Agogo, Ghana Dunkwa Government Hospital Dunkwa, Ghana Nkawie-Toase Government Hospital Nkawie, Ghana Tepa Government Hosital Tepa, Ghana 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.32mL 0.46mL 0.23mL |
11.59mL 2.32mL 1.16mL |
23.17mL 4.63mL 2.32mL |
CAS号 | 294646-77-8 |
分子式 | C24H29N7O |
分子量 | 431.533 |
别名 | (R)-CR8;CR8, (R)-Isomer |
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: 50 mg/mL(115.87 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 |