pim1

Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.

CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).

XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. XL-413 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induct

TCS PIM-1 1 (SC 204330)(sc-204330) is an effective and specific ATP-competitive Pim-1 kinase inhibitor (IC50: 50 nM), exhibiting good specificity over MEK1/MEK2 and Pim-2 (IC50s > 20,000 nM).

(Z)-SMI-4a (TCS PIM-1 4a) is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM.

SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM).

TCS-PIM-1-4a (SMI-4a), a Pim inhibitor, blocks mTORC1 activity through activation of AMPK and kills a wide range of both myeloid and lymphoid cell lines (IC50=0.8-40 μM).

XL413 hydrochloride (BMS-863233 Hydrochloride) is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC 50 of 3.4 nM. XL413 hydrochloride also exhibits potent effect with IC 50 s of 215, 42 nM on CK2, PIM1, respectively, and an EC 50 of 118 nM on pMCM.

XL413 HCl is an ATP-competitive Cdc7 inhibitor (IC50: 3.4 nM) that is potent and selective.XL413 HCl inhibited CK2 and PIM1 with IC50 values of 215 and 42 nM, respectively.XL413 HCl showed an EC50 value of 118 against pMCM.

Quercetagetin (6-Hydroxyquercetin) (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu. It is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50: 0.34 μM).

Hispidulin, a natural flavone with a broad spectrum of biological activities, is a Pim-1 inhibitor (IC50: 2.71 μM).

CK2 PIM1-IN-1 is an inhibitor of CK2 (IC50: 3.787 μM) and PIM1 (IC50: 4.327 μM), developed for researching proliferative disorders like cancer and other kinase-associated conditions.

PIM1-IN-1 is a potent and highly selective inhibitor of PIM1 3 (IC50s: 7 nM for PIM1, 5530 nM for PIM2, and 70 nM for PIM3) with antiproliferative and anti-cancer activity.

CDK2/PIM1-IN-1 is an inhibitor of the kinases CDK2 (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM). It can induce apoptosis (cell death) and reduce the expression of TNF-α, which promotes tumors. CDK2/PIM1-IN-1 exhibits antitumor activity.

PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor with an IC50 of 0.67 μM, and it also shows notable cytotoxicity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively [1].

PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor with an IC50 of 0.60 μM and exhibits high cytotoxicity on HCT-116 and MCF-7 cells, with IC50 values of 1.51 μM and 15.2 μM, respectively.

CDK6/PIM1-IN-1 is a balanced, potent dual inhibitor of CDK6 (IC50: 39 nM) and PIM1 (IC50: 88 nM), also showing inhibitory activity on CDK4 (IC50: 3.6 nM). It significantly inhibits the proliferation of acute myeloid leukemia (AML) cells, arrests the cell cycle in G1 phase, induces cell apoptosis, and demonstrates anti-AML activity.

PIM1-IN-3 (Compound HL8) is a potent, selective PIM-1 enzyme inhibitor that effectively induces apoptosis in Colo320 cells, demonstrating significant research potential for cancer diseases.

PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1 and also shows significant inhibitory activity against SGK-1, PKA, CaMK-1, GSK3β, and MSK1, making it potentially valuable for cancer research [1].

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and potential anticancer activity, and inhibits DPPH.Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits the growth of PC-3 cells with an IC50 value of 16 nM. Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used in prostate cancer research.

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1 2 3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.