Briciclib is a small molecule that suppresses cyclin D1 accumulation in cancer cells.
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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 |
SGK,ERK | 99%+ | ||||||||||||||||
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 | 99%+ | |||||||||||||||
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(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM |
99%+ | |||||||||||||||||
A-674563 HCl |
++
CDK2, Ki: 46 nM |
PKA | 99%+ | ||||||||||||||||
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 |
99%+ | |||||||||||||||
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 | 99%+ | ||||||||||||
(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/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/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 |
99%+ | ||||||||||||||||
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 | Briciclib targets eIF4E and inhibits the proliferation of various cancer cell lines including mantle cell leukemia, breast, gastric, and esophageal cancers with GI50 values of 9.8-12.2 nM, without affecting normal endothelial cells. It also reduces the expression of cyclin D1 and c-Myc in cancer cell lines within 8 hours[1]. |
体外研究 | Briciclib targets eIF4E and inhibits the proliferation of various cancer cell lines including mantle cell leukemia, breast, gastric, and esophageal cancers with GI50 values of 9.8-12.2 nM, without affecting normal endothelial cells. It also reduces the expression of cyclin D1 and c-Myc in cancer cell lines within 8 hours[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.11mL 0.42mL 0.21mL |
10.54mL 2.11mL 1.05mL |
21.08mL 4.22mL 2.11mL |
CAS号 | 865783-99-9 |
分子式 | C19H23O10PS |
分子量 | 474.419 |
别名 | ON 014185 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 30 mg/mL(63.24 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 |