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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...

化合物

BGG463
Cat.No: T4618
Synonym: K 0859
Target: Bcr-Abl, CDK
AUZ 454
Cat.No: T6866
Synonym: K03861
Target: CDK
HQ461
Cat.No: T9849
Synonym:
Target: CDK, Molecular Glues
dCeMM3 
Cat.No: T9758
Synonym: 2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide
Target: Others
dCeMM2
Cat.No: T61477
Synonym:
Target: Molecular Glues
2,5-dimethyl Celecoxib
Cat.No: T35610
Synonym:
Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor
dCeMM4
Cat.No: T61057
Synonym:
Target:
PP-C8
Cat.No: T74359
Synonym:
Target: PROTACs
NCT02
Cat.No: T60030
Synonym:
Target:
SR-1277
Cat.No: T38927
Synonym:
Target:
OTS964
Cat.No: T61800
Synonym:
Target:
6-Chloro-2-fluoropurine
Cat.No: T37065
Synonym:
Target:
CDK-IN-9
Cat.No: T62235
Synonym:
Target:
Inostamycin A
Cat.No: T36844
Synonym:
Target:
TargetMol Loading
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