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41

抑制剂 & 化合物

1

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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

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

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

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

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

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 CDK8CDK19 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

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(CDK8CDK19,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、CDK8CDK7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 8CDK19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 CDK8CDK19 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CDK8CDK19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

JH-VIII-49 is an effective and selective inhibitor of CDK8.
T23909 Cortistatin A

Cortistatin-A

Cortistatin A is a potent and selective mediator-associated kinase CDK8 and its paralogue CDK19 inhibitor.
T61590 DS96432529

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

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

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。

化合物

CDK8-IN-13
Cat.No: T72029
Synonym:
Target: Apoptosis, CDK
CDK8-IN-1
Cat.No: T10740
Synonym:
Target: CDK
CDK8-IN-12
Cat.No: T72048
Synonym:
Target: GSK-3, CDK
CDK8-IN-4
Cat.No: T17305
Synonym:
Target: CDK
CDK8-IN-3
Cat.No: T14917
Synonym:
Target: Others
CDK8/19-IN-1
Cat.No: T10739
Synonym:
Target: CDK
CDK8-IN-4k
Cat.No: T70148
Synonym:
Target:
CDK8-IN-9
Cat.No: T64245
Synonym:
Target:
CDK8-IN-18
Cat.No: T70098
Synonym:
Target:
CDK8-IN-10
Cat.No: T63690
Synonym:
Target:
CDK8-IN-5
Cat.No: T62310
Synonym:
Target:
CDK8-IN-11 hydrochloride
Cat.No: T62293
Synonym:
Target:
CDK8-IN-6
Cat.No: T62112
Synonym:
Target:
CDK8-IN-7
Cat.No: T62354
Synonym:
Target:
CDK8-IN-11
Cat.No: T61742
Synonym:
Target:
Fipravirimat
Cat.No: T70147
Synonym:
Target:
BRD6989
Cat.No: T14778
Synonym:
Target: IL Receptor, CDK, Interleukin
NU1085
Cat.No: T71908
Synonym:
Target:
3MB-PP1
Cat.No: T21678
Synonym:
Target: PLK
CCT-251921
Cat.No: T14901
Synonym:
Target: CDK
SEL120-34A
Cat.No: T10744
Synonym:
Target: CDK
Senexin B
Cat.No: T8430
Synonym: 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
Target: CDK
SEL120-34A HCl
Cat.No: T10744L
Synonym:
Target: CDK
Senexin C
Cat.No: T62702
Synonym:
Target: CDK
MSC2530818
Cat.No: TQ0266
Synonym:
Target: CDK
Senexin A
Cat.No: T5673
Synonym:
Target: CDK
LY2857785
Cat.No: TQ0060
Synonym:
Target: Apoptosis, CDK
BI-1347
Cat.No: T5405
Synonym:
Target: CDK
AS2863619
Cat.No: T8378
Synonym:
Target: CDK, STAT
CCT251545
Cat.No: T14907
Synonym:
Target: Wnt/beta-catenin
JH-XVI-178
Cat.No: T40280
Synonym:
Target:
JH-XI-10-02
Cat.No: T13743
Synonym:
Target: EGFR
SNX7886
Cat.No: T81137
Synonym:
Target: PROTACs
AS2863619 free base
Cat.No: T10382
Synonym:
Target: CDK
JH-VIII-49
Cat.No: T24200
Synonym: JH-VIII49,JH-VIII 49,JHVIII-49,JHVIII 49,JHVIII49
Target:
Cortistatin A
Cat.No: T23909
Synonym: Cortistatin-A
Target:
DS96432529
Cat.No: T61590
Synonym:
Target:
SNX2-1-108
Cat.No: T24811
Synonym: SNX-21108,SNX21108,SNX 21108
Target:
CCT251545 analogue, Compound 51
Cat.No: T22633
Synonym:
Target: Others
UNC10112785
Cat.No: T68758
Synonym:
Target:
LL-K8-22
Cat.No: T74784
Synonym:
Target:
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。

天然产物

Wogonin
Cat.No: T2933
Synonym: Vogonin,汉黄芩素
Target: Apoptosis, Wnt/beta-catenin, CDK, Autophagy
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