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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T72029 |
CDK8-IN-13
|
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
CDK8-IN-13是一种 CDK8抑制剂(IC50:51.9 nM),具有强效性、选择性和口服活性。CDK8-IN-13能诱导细胞凋亡,降低了 p-STAT1 S727和p-STAT5 S726的表达。CDK8-IN-13表现出抗肿瘤活性。 | |||
T10740 |
CDK8-IN-1
|
CDK | Cell Cycle/Checkpoint |
CDK8-IN-1 是一个有效的、CDK8 的选择性抑制剂,其 IC50 值为 3 nM。 | |||
T72048 |
CDK8-IN-12
|
GSK-3; CDK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
CDK8-IN-12 是一种具有选择性、有效性和口服活性的 CDK8 抑制剂(Ki : 14 nM),是一种抗癌剂。CDK8-IN-12 对 GSK-3α、GSK-3β、PCK-θ 具有抑制作用,Ki 分别为 13 nM、4 nM、109 nM。CDK8-IN-12对 MV4-11 细胞显示出抗增殖活性。 | |||
T17305 |
CDK8-IN-4
|
CDK | Cell Cycle/Checkpoint |
CDK8-IN-4 is an inhibitor of CDK8 (IC50: 0.2 nM). | |||
T14917 |
CDK8-IN-3
|
Others | Others |
CDK8-IN-3 is an inhibitor of CDK8. | |||
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). | |||
T70148 |
CDK8-IN-4k
|
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CDK8-IN-4k is a potent and highly selective CDK8 inhibitor, with no apparent potential for time-dependent CYP3A4 inhibition. | |||
T64245 | CDK8-IN-9 | ||
CDK8-IN-9 (compound 22) 是一种 II 型 CDK8 的有效抑制剂 (IC50: 48.6 nM),对肿瘤生长表现出抑制作用。CDK8-IN-9 能够用于研究结直肠癌。 | |||
T70098 |
CDK8-IN-18
|
||
CDK8-IN-18, also known as ZINC584617986, is a potent and selective inhibitor of CDK8, also modulating CDK19. | |||
T63690 |
CDK8-IN-10
|
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CDK8-IN-10 是选择性的、有效的细胞周期蛋白依赖性激酶 (CDK8) 抑制剂 (IC50: 8.25 nM),能够用于研究癌症。 | |||
T62310 | CDK8-IN-5 | ||
CDK8-IN-5 是一种有效的 CDK8抑制剂,IC50为 72 nM。CDK8-IN-5 显示抗炎活性和 43% 的 IL-10增强率。CDK8-IN-5 具有研究炎症性肠病的潜力。 | |||
T62293 | CDK8-IN-11 hydrochloride | ||
CDK8-IN-11 hydrochloride 是一种选择性、有效的 CDK8 抑制剂 (IC50: 46 nM)。CDK8-IN-11 hydrochloride 对 WNT/β-catenin 信号通路具有抑制作用。CDK8-IN-11 hydrochloride 能够用于研究结肠癌。 | |||
T62112 |
CDK8-IN-6
|
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CDK8-IN-6 (compound 9) 是一种细胞周期蛋白依赖性激酶8 (CDK8) 的有效抑制剂 (Kd: 13 nM)。CDK8-IN-6 对 MOLM-13、OCI-AML3、MV4-11、NRK 和 H9c2 细胞表现出细胞毒性,他们 IC50s 分别为 11.2、7.5、8.6、20.5、12.5-25 μM。CDK8-IN-6 对 AML 癌症表现出潜在的研究价值。 | |||
T62354 |
CDK8-IN-7
|
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CDK8-IN-7 (compound 12) 是一种有效的、选择性的细胞周期蛋白依赖性激酶 8 (CDK8) 抑制剂 (Kd: 3.5 nM)。CDK8-IN-7 对 MOLM-13 细胞 (IC50: 5.9 μM)、OCI-AML3 细胞 (IC50: 4.8 μM)、MV4-11 细胞 (IC50: 5.4 μM)、NRK 细胞 (IC50: 16.2 μM) 和 H9c2 细胞 (IC50: 12.5-25 μM) 具有细胞毒性。CDK8-IN-7 对 AML-癌症表现出研究潜力。 | |||
T61742 | CDK8-IN-11 | ||
CDK8-IN-11是一种高效且选择性的CDK8抑制剂,其IC50为46 nM。该化合物能够抑制WNT/β-catenin信号通路,主要用于结肠癌研究。 | |||
T70147 |
Fipravirimat
|
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Fipravirimat 是一种有效的 HIV-1抑制剂。Fipravirimat 具有用于HIV 和 AIDS 研究的潜力。 | |||
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。 | |||
T71908 |
NU1085
|
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NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h. | |||
T21678 |
3MB-PP1
|
PLK | Cell Cycle/Checkpoint |
3MB-PP1是嘌呤类似物,是一种 Polo 样激酶 1 (Plk1) 抑制剂。在表达类似物敏感的 Plk1 等位基因的细胞中,3MB-PP1 通过靶向 Plk1 阻断有丝分裂进程和细胞分裂。3MB-PP1 特异性抑制类似物敏感的 Ssn3 (Cdk8)。3MB-PP1 抑制 Leu93 突变 Zipper-interacting protein kinase(Leu93-ZIPK),IC50为2 μM。3MB-PP1 可用于细胞分裂和白色念珠菌 (Candida albicans) 菌丝形成的研究。 | |||
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。 | |||
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。 | |||
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)。 | |||
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。 | |||
T62702 | Senexin C | CDK | Cell Cycle/Checkpoint |
Senexin C 是一种新型具有口服活性和特异性的 CDK8/19 抑制剂,具有潜在的抗癌活性。Senexin C 比 Senexin B的代谢更稳定,作用效果更强。Senexin C 抑制 MV4-11 白血病细胞的生长。 | |||
TQ0266 |
MSC2530818
|
CDK | Cell Cycle/Checkpoint |
MSC2530818 是一种有效的、选择性的、可口服的 CDK8 抑制剂,IC50值为2.6 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。 | |||
TQ0060 |
LY2857785
|
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
LY2857785 是 I 型可逆的 ATP 竞争性 CDK9、CDK8和 CDK7抑制剂,IC50分别为 11 nM、16 nM 和 246 nM。 | |||
T5405 |
BI-1347
|
CDK | Cell Cycle/Checkpoint |
BI-1347 是一种有效的、选择性的 CDK8/cyclinC 抑制剂,IC50值为 1 nM,可抑制肿瘤生存。 | |||
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。 | |||
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. | |||
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. | |||
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%。 | |||
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. | |||
T24200 |
JH-VIII-49
JH-VIII49,JH-VIII 49,JHVIII-49,JHVIII 49,JHVIII49 |
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JH-VIII-49 is an effective and selective inhibitor of CDK8. | |||
T23909 |
Cortistatin A
Cortistatin-A |
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Cortistatin A is a potent and selective mediator-associated kinase CDK8 and its paralogue CDK19 inhibitor. | |||
T61590 |
DS96432529
|
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DS96432529 是一种具有口服活性和CDK8抑制活性的强效骨合成代谢剂。 | |||
T24811 |
SNX2-1-108
SNX-21108,SNX21108,SNX 21108 |
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SNX2-1-108 is a selective CDK8 and CDK19 inhibitor. | |||
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 | |||
T68758 |
UNC10112785
|
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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. | |||
T74784 | LL-K8-22 | ||
LL-K8-22 是一款高效且具有选择性和持久性的 CDK8-cyclin C 双重降解剂,其DC50值分别为2.52 μM和2.64 μM。该化合物还能抑制STAT1Ser 727的磷酸化,并能抑制由E2F 和 MYC 驱动的致癌转录程序,适用于三阴性乳腺癌 (TNBC) 的研究。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2933 |
Wogonin
Vogonin,汉黄芩素 |
Apoptosis; Wnt/beta-catenin; CDK; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Wogonin (Vogonin) 是一种具有细胞渗透性的口服类黄酮,具有抗炎和抗癌特性,能够抑制 CDK8和 Wnt 的活性。 |