HQ461是一种分子粘合降解剂,通过促进 CDK12 与 DDB1-CUL4-RBX1 E3 泛素连接酶的相互作用,导致 CDK12 相关蛋白 Cyclin K(CCNK)的多泛素化和降解。
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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 | 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(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 |
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 | 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/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 |
99% | ||||||||||||||||
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 |
++
Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM |
99%+ | |||||||||||||||||
(E/Z)-TG003 |
+++
mCLK4, IC50: 15 nM mCLK1, IC50: 200 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 | HQ461 is a molecular glue that enhances the interaction between CDK12 and DDB1, leading to the degradation of cyclin K. This degradation disrupts CDK12 activity, reducing phosphorylation of its substrates, downregulating DNA damage response genes, and inducing cell death[1]. |
体外研究 | HQ461 reduces the viability of A549 cells with an IC50 of 1.3 µM[1]. HQ461, at a concentration of 10 µM for 8 hours, lowers the level of CDK12 protein in A549 cells[1]. HQ461 facilitates the association of CDK12/CCNK with DDB1 in A549 cells across a concentration range of 0 to 10 µM[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.89mL 0.58mL 0.29mL |
14.47mL 2.89mL 1.45mL |
28.95mL 5.79mL 2.89mL |
CAS号 | 1226443-41-9 |
分子式 | C15H15N5OS2 |
分子量 | 345.442 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解方案 |
DMSO: 60 mg/mL(173.69 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 |