Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4618 |
BGG463
K 0859 |
Bcr-Abl; CDK | Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
BGG463 (K 0859) 是一种具有口服活性的 II 型 CDK2的抑制剂,可抑制 c-ABL-T334I、BCR-ABL 和 BCR-ABL-T315I 变体,IC50分别为 0.25 μM、0.09 μM 和 0.590 μM。 | |||
T6866 |
AUZ 454
K03861 |
CDK | Cell Cycle/Checkpoint |
AUZ 454 (K03861) 是一种 II 型 CDK2 抑制剂,Kd 值是 8.2 nM。它对 CDK2(WT)、CDK2(C118L)、CDK2(A144C) 和 CDK2(C118L/A144C) 的 Kd 分别为 50 nM、18.6 nM、15.4 nM 和 9.7 nM。 | |||
T9849 |
HQ461
|
CDK; Molecular Glues | Cell Cycle/Checkpoint; PROTAC |
HQ461 是一种分子胶,可促进 CDK12-DDB1 相互作用并触发 cyclin K 降解, cyclin K 的降解会损害 CDK12 的功能,导致 CDK12 底物磷酸化降低、DNA 损伤反应基因下调和细胞死亡。 | |||
T9758 |
dCeMM3
2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide |
Others | Others |
dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) 是一种胶降解剂,可以诱导 cyclin K 的泛素化和降解。机制是通过促进 CDK12-cyclin K 与 CRL4B 连接酶复合物的相互作用。 | |||
T61477 |
dCeMM2
|
Molecular Glues | PROTAC |
dCeMM2 (Compound 2) 是一种胶降解剂。dCeMM2 促使 CDK12-cyclin K 与 CRL4B 连接酶复合物的相互作用,导致 cyclin K 的泛素化及降解。 | |||
T35610 |
2,5-dimethyl Celecoxib
|
Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells |
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。 | |||
T61057 | dCeMM4 | ||
dCeMM4 (Compound 5) 是通过促进 CDK12-cyclin K 与 CRL4B 连接酶复合物的相互作用来诱导 cyclin K 的泛素化和降解的分子胶降解剂。 | |||
T74359 |
PP-C8
|
PROTACs | PROTAC |
PP-C8 是一种有效的选择性 PROTACCDK12-Cyclin K 降解剂。PP-C8 诱导 CDK12-Cyclin K 降解,对 CDK12 和 Cyclin K 的DC50分别为 416 和 412 nM。PP-C8 与PARP 抑制剂在三阴性乳腺癌 (TNBC) 中具有高效的协同抗增殖作用。 | |||
T60030 | NCT02 | ||
NCT02 是一种细胞周期蛋白 K 降解剂,可诱导细胞周期蛋白 K (CCNK) 的泛素化和 CCNK 及其复合物 CDK12 的蛋白酶体降解。NCT02具有研究转移性结直肠癌 (CRC) 的潜力。 | |||
T38927 |
SR-1277
|
||
SR-1277 is a highly potent, selective, and ATP competitive inhibitor of CK1δ/ε, with IC50 values of 49 nM and 260 nM, respectively. Additionally, SR-1277 exhibits inhibitory effects on FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K, with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. Taken together, SR-1277 represents a valuable tool for cancer research. | |||
T61800 |
OTS964
|
||
OTS964 is a potent, orally active compound that operates as a highly selective inhibitor of TOPK with an IC 50 of 28 nM [1]. Additionally, it demonstrates significant inhibitory action against cyclin-dependent kinase CDK11, specifically binding to CDK11B with a K d of 40 nM [2]. | |||
T37065 |
6-Chloro-2-fluoropurine
|
||
6-Chloro-2-fluoropurine is a heterocyclic building block.1,2It has been used in the synthesis of purine nucleosides that inhibit cyclin-dependent kinases (CDKs)in vitro.16-Chloro-2-fluoropurine has also been used in the synthesis of purine nucleosides that are active against HIV-1 and hepatitis B virus (HBV)in vitro.2 1.Wilson, S.C., Atrash, B., Barlow, C., et al.Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitorsBioorg. Med. Chem.19(22)6949-6965(2011) 2.... | |||
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)。 | |||
T36844 |
Inostamycin A
|
||
Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes) and is selective for CDP-diacylglycerol:inositol 3-phosphatidyltransferase over phospholipase C (PLC) and phosphatidylinositol kinase at 10 μg/ml.2Inostamycin A decreases viability of YCU-T892, KCC-TC873, KB, HSC-4, and YCU-T891 oral squamous cell carcinoma (OSCC) cells in a con... |