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- 作用机制
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- Inhibitor (抑制剂) (96)
- Agonist (激动剂) (1)
- Degrader (降解剂) (1)
- 靶点
| Catalog No. | Inhibitor Name | CDK1 | CDK2 | CDK3 | CDK4 | CDK5 | CDK6 | CDK7 | CDK8 | CDK9 | CLK | CDK | Cdc | Other |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| A10701 | Palbociclib HCl | **** | *** | |||||||||||
| A10806 | Roscovitine | * | ** | * | ERK2,GST-ERK1,ERK1 | |||||||||
| A10850 | SNS-032 | * | *** | * | * | ** | **** | GSK-3α,GSK-3β | ||||||
| A11129 | Dinaciclib | **** | **** | **** | **** | |||||||||
| A10390 | Flavopiridol | *** | *** | *** | ** | * | ||||||||
| A10093 | AT7519 | ** | ** | ** | *** | ** | * | **** | GSK-3β | |||||
| A11045 | Flavopiridol HCl | *** | *** | * | *** | *** | * | |||||||
| A10494 | JNJ-7706621 | **** | **** | * | ** | Aurora A,Aurora B,VEGFR2 | ||||||||
| A11105 | AZD5438 | *** | **** | ** | *** | |||||||||
| A11167 | MK-8776 | ** | Chk1,Chk2 | |||||||||||
| A10716 | PHA-793887 | ** | **** | ** | **** | **** | ** | GSK-3β | ||||||
| A10163 | BS-181 HCl | *** | ||||||||||||
| A13811 | Palbociclib Isethionate | **** | *** | |||||||||||
| A11034 | A-674563 | ** | Akt1,PKA,GSK-3β | |||||||||||
| A16386 | abemaciclib | **** | **** | |||||||||||
| A11154 | BMS-265246 | **** | **** | ** | ||||||||||
| A11164 | PHA-767491 | ** | ** | * | *** | **** | **** | GSK-3β,MK2,PLK1 | ||||||
| A11047 | Milciclib | * | *** | ** | * | ** | TrkA | |||||||
| A11190 | R547 | **** | **** | **** | GSK-3β | |||||||||
| A14136 | NU6027 | * | * | ATR,DNA-PK | ||||||||||
| A13547 | P276-00 | ** | ** | ** | * | * | *** | GSK-3β,PKCα,c-Src | ||||||
| A11220 | Kenpaullone | * | * | * | GSK-3β,ERK2,c-Src | |||||||||
| A15889 | K03861 | **** | ||||||||||||
| A14192 | THZ1 | **** | ||||||||||||
| A11313 | AT7519 HCl | ** | ** | * | ** | *** | ** | * | **** | GSK-3β | ||||
| A15517 | Purvalanol A | *** | * | **** | ||||||||||
| A14437 | Ro-3306 | *** | PKCδ,SGK,ERK | |||||||||||
| A14318 | SU9516 | *** | *** | ** | PDGFR | |||||||||
| A13677 | XL413 | **** | **** | Pim1,CK2 | ||||||||||
| A14273 | LDC000067 | * | * | * | *** | |||||||||
| A14297 | ML167 | ** | ||||||||||||
| A13721 | TG003 | *** | ||||||||||||
| A13549 | Ribociclib | |||||||||||||
| A12216 | Wogonin | |||||||||||||
| A10471 | Indirubin | * | GSK-3β | |||||||||||
| A11347 | CGP60474 | *** | *** | PKCα | ||||||||||
| A12352 | Purvalanol B | **** | **** | |||||||||||
| A12438 | NU 6102 | *** | **** | * | ||||||||||
| A12989 | LY2835219 (abemaciclib) | **** | *** | |||||||||||
| A14025 | AMG-925 | * | **** | FLT3 | ||||||||||
| A15054 | CVT 313 | * | * | * | ||||||||||
| A15196 | NVP-LCQ195 | **** | *** | **** | CHK2 | |||||||||
| A15767 | NU2058 | * | * | DNA topoisomerase II ATPase | ||||||||||
| A15823 | LY2857785 | * | *** | *** |
Notes:
1.Hover mouse over "" to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of "" is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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RGB-286638
Catalog No. A13130 CDK 抑制剂RGB-286638是一种新型CDK抑制剂，对于细胞周期蛋白T1-CDK9/细胞周期蛋白B1-CDK1/细胞周期蛋白E-CDK2/细胞周期蛋白D1-CDK4/细胞周期蛋白E-CDK3的IC50为1 nM/2 nM/3 nM/4 nM/5 nM/p35-CDK5分别；对细胞周期蛋白H-CDK7和细胞周期蛋白D3-CDK6的效力较低。 了解更多 -
THAL-SNS-032
Catalog No. A19088 CDK9 degrader PROTACTHAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN). 了解更多 -
AT7519 trifluoroacetate
Catalog No. A15005 CDK 抑制剂AT7519 trifluoroacetate是CDK1、2、4、6和9的多CDK抑制剂，IC50为10-210 nM，对CDK3的效力较低，对CDK7的活性较低。 了解更多 -
FMF-04-159-2
Catalog No. A18911 CDK14 inhibitorFMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively. 了解更多 -
Abemaciclib Metabolites M2
Catalog No. A18416 CDK4/CDK6 inhibitorAbemaciclib Metabolites M2 is a metabolite of abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity. 了解更多 -
CDK9 inhibitor 2
Catalog No. A15039 -
NSC 663284
Catalog No. A13524 Cdc25 抑制剂NSC 663284是所有Cdc25同工型的有效，细胞可渗透且不可逆的抑制剂，首选Cdc25A（对于Cdc25A，Cdc25B2和Cdc25C，IC50分别为29、95和89 nM）。 了解更多 -
MSC2530818
Catalog No. A12644 CDK8 inhibitorMSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8. 了解更多 -
CA-224
Catalog No. A14414 -
CDK4/6-IN-2
Catalog No. A18657 CDK4/CDK6 inhibitorCDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor with IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively. 了解更多 -
Lerociclib (G1T38)
Catalog No. A18320 CDK inhibitorLerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively. 了解更多 -
Trilaciclib
Catalog No. A17084 -
SEL120-34A
Catalog No. A17086 -
PF-06873600
Catalog No. A16875 CDK 抑制剂PF-06873600是一种口服生物利用型，细胞周期蛋白依赖性激酶（CDK）抑制剂，其对 CDK2、CDK4和CDK6的Ki值分别为 0.09 nM、0.13 nM 和 0.16 nM。具有潜在的抗肿瘤活性。 了解更多 -
ICEC0942 HCl
Catalog No. A16903 CDK7 抑制剂ICEC0942 HCl，也称为CT7001，是CDK7的口服生物利用选择性抑制剂。它选择性抑制CDK7，IC50为40nM。CDK1，CDK2，CDK5和CDK9的IC50值分别高45倍，15倍，230倍和30倍。 了解更多 -
Atuveciclib (BAY-1143572)
Catalog No. A16810 Selective PTEFb/CDK9 抑制剂Atuveciclib (BAY-1143572)是目前处于I期的PTEFb/CDK9的高度选择性，有效且可口服的抑制剂。 了解更多 -
SB1317 (TG02)
Catalog No. A13454 CDK/JAK2/FLT3 抑制剂SB1317是细胞周期蛋白依赖性激酶（CDKs）、类FMS酪氨酸激酶-3（FLT3）和Janus激酶2（JAK2）的有效抑制剂，CDK2、JAK2和FLT3的IC50值分别为13nM、56nM和73nM。 了解更多 -
LY2835219 methanesulfonate
Catalog No. A16386 -
Bohemine
Catalog No. A15942 -
Flavopiridol HCl
Catalog No. A11045 -
JNJ-7706621
Catalog No. A10494 CDK/Aurora A/B 抑制剂JNJ-7706621是对CDK1/2具有最高效力的pan-CDK抑制剂，IC50为9 nM/4 nM，并且在无细胞分析中对CDK1/2的选择性是CDK3/4/6的6倍以上。它还能有效抑制极光A/B，对Plk1和Wee1没有活性。 了解更多 -
PHA-848125 (Milciclib)
Catalog No. A11047 CDK 抑制剂PHA-848125 (Milciclib)是一种有效的，ATP竞争性CDK抑制剂，作用于CDK2，IC50为45 nM，作用于CDK2比作用于CDK1，2，4，5和7选择性高3倍以上。 了解更多 -
AZD5438
Catalog No. A11105 -
BMS-265246
Catalog No. A11154 -
SNS-032 (BMS-387032)
Catalog No. A10850 CDK 抑制剂SNS-032（BMS-387032）是细胞周期蛋白依赖性激酶（Cdks）2、7和9的高度选择性和有效抑制剂，具有体外生长抑制作用，并具有诱导恶性B细胞凋亡的能力。 了解更多 -
AT7519 HCl
Catalog No. A11313 -
Purvalanol B
Catalog No. A12352 CDK 抑制剂Purvalanol B是一种细胞周期蛋白依赖性激酶抑制剂。对于cdc2/cyclin B，cdk2/cyclin A，cdk2/cyclin E，cdk4/cyclin D1和cdk5-p35的ic50值分别为6、6、9、> 10，000和6 nm。对一系列其他蛋白激酶具有选择性(IC50 > 10，000 nM)。 了解更多