Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T14778 |
BRD6989
|
IL Receptor; CDK; Interleukin | Cell Cycle/Checkpoint; Immunology/Inflammation |
BRD6989 是天然产物皮质抑素 A 的类似物,可抑制CDK8并上调IL-10,抑制重组 CDK8 或 CDK19 复合物的激酶活性。它选择性结合 CDK8 复合物,IC50约为 200 nM。 | |||
T8430 |
Senexin B
4-[[2-[6-[(4-甲基-1-哌嗪基)羰基]-2-萘基]乙基]氨基]-6-喹唑啉甲腈 |
CDK | Cell Cycle/Checkpoint |
Senexin B 是一种有效的选择性 CDK8/19 抑制剂(CDK8 和 CDK19,Kd 分别为 140 nM 和 80 nM)。 | |||
T5673 |
Senexin A
|
CDK | Cell Cycle/Checkpoint |
Senexin A 是一种有效且选择性的 CDK8 抑制剂,它还抑制 CDK19,Kd 值分别为0.83μM 和0.31μM。 | |||
T10744 |
SEL120-34A
|
CDK | Cell Cycle/Checkpoint |
SEL120-34A 是CDK8的选择性和ATP 竞争性抑制剂,对CDK8/CycC、CDK19/CycC 和CDK9/cycT 的IC50s 为4.4 nM、10.4 nM 和1070 nM。SEL120-34A 具有抗肿瘤活性。 | |||
T10744L |
SEL120-34A HCl
|
CDK | Cell Cycle/Checkpoint |
SEL120-34A HCl 是一种可口服的,选择性的,ATP-竞争性的CDK8抑制剂,具有抗肿瘤活性,对 CDK8/CycC 和 CDK19/CycC 的IC50值分别为 4.4 nM 和 10.4 nM。 | |||
T8378 |
AS2863619
|
CDK; STAT | Cell Cycle/Checkpoint; JAK/STAT signaling; Stem Cells |
AS2863619 是一种口服的细胞周期蛋白依赖性激酶 8 和CDK19抑制剂,抑制CDK8/19可增强STAT5的激活,从而激活 Foxp3 基因。它可将抗原特异性效应子/记忆 T 细胞转换为 Foxp3+调节性 T 细胞,以研究各种免疫疾病。 | |||
T14907 |
CCT251545
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
CCT251545 是一种有效的、具有口服活性的WNT 抑制剂,在 7dF3 细胞中对 WNT 抑制作用的IC50值为 5 nM。它是选择性化学探针,用于探索 CDK8 和 CDK19 在人类疾病中的作用。 | |||
T10739 | CDK8/19-IN-1 | CDK | Cell Cycle/Checkpoint |
CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9). | |||
T81137 |
SNX7886
|
PROTACs | PROTAC |
SNX7886为高效CDK8/19蛋白降解剂,在293细胞中可分别降解CDK8与CDK19至90%及80%。 | |||
T70098 |
CDK8-IN-18
|
||
CDK8-IN-18, also known as ZINC584617986, is a potent and selective inhibitor of CDK8, also modulating CDK19. | |||
T23909 |
Cortistatin A
Cortistatin-A |
||
Cortistatin A is a potent and selective mediator-associated kinase CDK8 and its paralogue CDK19 inhibitor. | |||
T14901 |
CCT-251921
|
CDK | Cell Cycle/Checkpoint |
CCT-251921是一种有口服活性的选择性CDK8抑制剂;IC50值为2.3 nM。 | |||
T24811 |
SNX2-1-108
SNX-21108,SNX21108,SNX 21108 |
||
SNX2-1-108 is a selective CDK8 and CDK19 inhibitor. | |||
T10382 |
AS2863619 free base
|
CDK | Cell Cycle/Checkpoint |
AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene. | |||
T68758 |
UNC10112785
|
||
UNC10112785 is a novel potent inhibitor of CDK8, CDK19, and CDK9 with IC50 at 1.05, 2.67, and 19.9 nM, respectively, causing MYC loss through both transcriptional and posttranslational mechanisms, and suppressing PDAC anchorage-dependent and anchorage-independent growth, inducing the substantial loss of MYC protein in both two-dimensional (2D) and 3D cell cultures. | |||
T13743 |
JH-XI-10-02
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. JH-XI-10-02 is a potent and selective degrader of CDK8, with an IC50 of 159 nM, based on PROTAC. | |||
T22633 |
CCT251545 analogue, Compound 51
|
Others | Others |
CCT251545 analog is a potent and selective CDK8/19 inhibitor (IC50: 5.1 nM and 5.6 nM, respectively). Mediator complex-associated kinases CDK8 and CDK19 are involved in the regulation of multiple transcription pathways. CDK8 plays as an oncogene in gastri | |||
T40280 | JH-XVI-178 | ||
JH-XVI-178 is a highly potent and selective CDK8/19 inhibitor with favorable pharmacokinetic attributes, including low clearance and moderate oral bioavailability. |