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9

抑制剂 & 化合物

1

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Cat. No. Product Name Target Signaling Pathways
TQ0078 CDK-IN-2

CDK inhibitor II

CDK Cell Cycle/Checkpoint
CDK-IN-2 (CDK inhibitor II) 是一种有效且特异性的 CDK9 抑制剂,IC50小于8 nM。
T36933 Cdk2 Inhibitor II

Cdk2 Inhibitor II,CDK2-IN-3

CDK Cell Cycle/Checkpoint
Cdk2 Inhibitor II 是一种具有选择性和有效性的 CDK2 抑制剂,50 为 60 nM。
T22461 YKL-5-124

CDK Cell Cycle/Checkpoint
YKL-5-124 是选择性不可逆CDK7共价抑制剂,对CDK7和CDK7/Mat1/CycH 的IC50分别为 53.5 nM 和 9.7 nM。它诱导强烈的细胞周期停滞,并抑制 E2F 驱动的基因表达。它对 CDK7 的生化和细胞选择性优于 CDK12/13。它对CDK7的选择性比 CDK9 和 CDK2 高 100 倍以上。
T8972 FIT-039

Others; DNA/RNA Synthesis; CDK; HSV Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others
FIT-039 是一种选择性和 ATP 竞争性的口服活性 CDK9 抑制剂,对CKD9/cyclin T1的IC50为 5.8 μM。它抑制HSV-1(IC50为 0.69 μM),HSV-2,人腺病毒和人CMV 的复制。它可抑制耐药性HSV 和其他 DNA 病毒,是有前途的抗病毒药物。
T3186 NU2058

O6-(Cyclohexylmethyl)guanine,O(6)-Cyclohexylmethylguanine

Topoisomerase; CDK Cell Cycle/Checkpoint; DNA Damage/DNA Repair
NU2058 (O(6)-Cyclohexylmethylguanine) 是一种基于鸟嘌呤的 CDK 抑制剂,抑制 CDK2 和 CDK1 的IC50值分别为 17 μM 和 26 μM。它也抑制 DNA 拓扑异构酶 II ATPase 活性,具有抗癌活性。
T6187 TDZD-8

GSK-3β Inhibitor I,NP 01139

GSK-3 PI3K/Akt/mTOR signaling; Stem Cells
TDZD-8 (NP 01139) 是抑制GSK-3β的抑制剂,其 IC50=2 μM。它对 Cdk-1/cyclin B,CK-II,PKA 和 PKC 的作用较弱,IC50值均 >100 μM。
T62235 CDK-IN-9

CDK-IN-9 (compound 24) 是一种 CDK 的有效抑制剂。CDK-IN-9 也是一种能够诱导 CDK12 和 DDB1 相互作用的分子胶, 能够作用于 CDK2/E (IC50: 4 nM) 。CDK-IN-9 能够导致细胞周期蛋白 K (cyclin K) 的多泛素化及其随后的降解。CDK-IN-9 可以利用去磷酸化视网膜母细胞瘤蛋白和RNA 聚合酶 II,进而诱导细胞凋亡 (apoptosis)。
T70988 Ibulocydine

Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7/cyclin H/Mat1 and Cdk9/cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibuloc...
T71549 RKS-262

RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several...

化合物

CDK-IN-2
Cat.No: TQ0078
Synonym: CDK inhibitor II
Target: CDK
Cdk2 Inhibitor II
Cat.No: T36933
Synonym: Cdk2 Inhibitor II,CDK2-IN-3
Target: CDK
YKL-5-124
Cat.No: T22461
Synonym:
Target: CDK
FIT-039
Cat.No: T8972
Synonym:
Target: Others, DNA/RNA Synthesis, CDK, HSV
NU2058
Cat.No: T3186
Synonym: O6-(Cyclohexylmethyl)guanine,O(6)-Cyclohexylmethylguanine
Target: Topoisomerase, CDK
TDZD-8
Cat.No: T6187
Synonym: GSK-3β Inhibitor I,NP 01139
Target: GSK-3
CDK-IN-9
Cat.No: T62235
Synonym:
Target:
Ibulocydine
Cat.No: T70988
Synonym:
Target:
RKS-262
Cat.No: T71549
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T17143 Toyocamycin

丰加霉素,Vengicide

Apoptosis; Others; IRE1; Antibiotic; Antifungal Apoptosis; Cell Cycle/Checkpoint; Microbiology/Virology; Others
Toyocamycin (Vengicide) 是放线菌类产生的腺苷类似物,为 X 盒结合蛋白 1 (XBP1) 抑制剂,抑制 IRE1α 诱导的 ATP 依赖性 XBP1 mRNA 的断裂,IC50值为 80 nM。它还诱导凋亡。

天然产物

Toyocamycin
Cat.No: T17143
Synonym: 丰加霉素,Vengicide
Target: Apoptosis, Others, IRE1, Antibiotic, Antifungal
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