Cdk2 Inhibitor II

Cdk2 Inhibitor II is a selective and potent CDK2 inhibitor50 at 60 nM.

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).

NU2058 (O(6)-Cyclohexylmethylguanine) is a guanine-based CDK inhibitor, also inhibits DNA topoisomerase II ATPase activity.

AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd values of 50 nM for CDK2(WT), 18.6 nM for CDK2(C118L), 15.4 nM for CDK2(A144C), and 9.7 nM for CDK2(C118L A144C).

CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).The inhibition of CDK9 induces apoptosis and potentiates the effect of cisplatin.

1-Naphthyl PP1 (1-NA-PP 1) is a selective Src inhibitor, targeting v-Src and c-Fyn, c-Abl, CDK2, and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18, and 22 μM, respectively.

Carbonic anhydrase inhibitor 14 (Compound 8b) is a potent CA inhibitor, exhibiting K i values of 1203, 99.7, 9.4, and 27.7 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. Additionally, it effectively inhibits CDK2 with an IC 50 of 20.3 μM and demonstrates significant antitumor activity [1].

CDK-IN-9 (compound 24) is a potent inhibitor of CDK and acts on CDK2 E (IC50: 4 nM). It functions as a molecular gel that induces interaction between CDK12 and DDB1, and can dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

CDK2-IN-11 (compound 9d) is a potent inhibitor of CDK2 (IC50: 6.4 μM) and acts on hCA II (Ki: 23.4 nM), hCA IX (Ki: 56.3 nM), and hCA XII (Ki: 44.3 nM). CDK2-IN-11 can be used in anticancer studies.

CDK2-IN-12 (compound 10b) is a potent inhibitor of CDK2 (IC50: 11.6 μM) and exhibits inhibition of hCA subtypes I, II, IX, and XII with KI values of 3534, 638.4, 44.3, and 48.8 nM, respectively. Additionally, CDK2-IN-12 shows anti-cancer effects.

EGFR-IN-45 is a potent pan-inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.4 μM and also targets CDK2 with an IC50 of 1.6 μM. It inhibits topoisomerases Topo I and Topo II, blocks the cancer cell cycle in the pre-G1 phase, and induces apoptosis.

YKL-5-124 TFA, a potent and selective irreversible covalent inhibitor of CDK7, demonstrates IC50 values of 53.5 nM for CDK7 and 9.7 nM for the CDK7 Mat1 CycH complex. It exhibits over 100-fold selectivity for CDK7 over CDK9 and CDK2, while showing no activity against CDK12 and CDK13. This compound effectively induces cell-cycle arrest, inhibits E2F-driven gene expression, and has minimal impact on the phosphorylation status of RNA polymerase II.

1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases v-Src.

Cdk2 Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, exhibits dose-dependent cytotoxic effects on U2OS osteosarcoma cells [1].

CDK7-IN-30 (Compound 22) is an inhibitor of CDK7 with an IC50 value of 7.21 nM, effectively inhibiting the phosphorylation of RNA polymerase II and CDK2. It can induce cell apoptosis (apoptosis) and exhibits anticancer activity, making it useful for cancer research.