PIM1
PIM1 is a constitutively active serine/threonine kinase that regulates cell survival, proliferation, cell-cycle progression, and apoptosis through phosphorylation of multiple downstream substrates involved in oncogenic signaling networks[1]. Mechanistically, PIM1 functions downstream of cytokine-responsive pathways, particularly JAK/STAT signaling, and cooperates with pathways including PI3K/AKT/mTOR, MYC, and NF-κB to promote cellular growth, metabolic adaptation, and resistance to stress signals[2][3]. In disease contexts, PIM1 is frequently overexpressed in hematologic malignancies, prostate cancer, and several solid tumors, where elevated activity is associated with tumor progression, survival advantages, and therapeutic resistance[3][4]. Experimental studies further demonstrate that PIM1 contributes to tumorigenicity, cellular migration, invasion, and maintenance of aggressive cancer phenotypes, supporting its value as a mechanistic target in cancer biology research[5][6]. Compared with the related isoforms PIM2 and PIM3, PIM1 shares a highly conserved catalytic domain and overlapping substrate specificity, yet displays distinct expression patterns and context-dependent biological functions that influence disease phenotypes and therapeutic responses[7][8]. For experimental applications, the unique ATP-binding pocket of PIM kinases has enabled development of selective and pan-PIM inhibitors, including SGI-1776, AZD1208, CX-6258, and TP-3654, which are widely used to investigate PIM-dependent signaling, proliferation, apoptosis, and drug-resistance mechanisms in preclinical models[3][7][9].
References:
- [1]. Uniprotkb.
- [2]. Gonzalez-Fajardo L, et al. Reduced in vivo toxicity of doxorubicin by encapsulation in cholesterol-containing self-assembled nanoparticles. Pharmacol Res. 2016 May;107:93-101. [Content Brief]
- [3]. Bellon M, et al. Targeting Pim kinases in hematological cancers: molecular and clinical review. Mol Cancer. 2023 Jan 25;22(1):18. [Content Brief]
- [4]. Luszczak S, et al. PIM kinase inhibition: co-targeted therapeutic approaches in prostate cancer. Signal Transduct Target Ther. 2020 Jan 31;5(1):7. [Content Brief]
- [5]. Wang J, et al. Pim1 kinase is required to maintain tumorigenicity in MYC-expressing prostate cancer cells. Oncogene. 2012 Apr 5;31(14):1794-803. [Content Brief]
- [6]. Santio NM, et al. PIM1 accelerates prostate cancer cell motility by phosphorylating actin capping proteins. Cell Commun Signal. 2020 Aug 8;18(1):121. [Content Brief]
- [7]. Mennati A, et al. Dual silencing of integrin αvβ3 receptor and insulin-like growth factor 1 receptor using mPEG-PCL/DDAB hybrid nanoparticle loaded siRNA in breast cancer therapy: An in vitro study on MCF-7 cells. Int J Biol Macromol. 2025 Mar;294:139334. [Content Brief]
- [8]. Rathi A, et al. Therapeutic targeting of PIM KINASE signaling in cancer therapy: Structural and clinical prospects. Biochim Biophys Acta Gen Subj. 2021 Nov;1865(11):129995. [Content Brief]
- [9]. Haddach M, et al. Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med Chem Lett. 2011 Dec 27;3(2):135-9. [Content Brief]
All Product Categories
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PIM1 Related Products (51)
Related Products (51)
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GSK-3β inhibitor 13
0 ImagesGSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease.
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AZD1897
0 ImagesAZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways.
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HS56
0 ImagesHS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension.
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CDK6/PIM1-IN-1
0 ImagesCat. No.: HY-142696CAS No.: 2677026-14-9CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.
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Pim-1 kinase inhibitor 11
0 ImagesCat. No.: HY-168071Pim-1 kinase inhibitor 11 (10f) is a PIM-1 inhibitor, with an IC50 of 0.18 μM. Pim-1 kinase inhibitor 11 (10f) exhibits anticancer activity. Pim-1 kinase inhibitor 11 (10f) induces apoptosis and arrests cell cycle progression.
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VS-II-173
0 ImagesCat. No.: HY-122670CAS No.: 1627962-21-3VS-II-173 is a pan-Pim kinase inhibitor with IC50 values of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPKα1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .
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CK2/PIM1-IN-1
0 ImagesCat. No.: HY-135816CAS No.: 292640-28-9CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.
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PIM1-IN-7
0 ImagesCat. No.: HY-147921CAS No.: 2439168-72-4PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor, with an IC50 of 0.67 μM. PIM1-IN-7 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively.
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KZ-02
0 ImagesCat. No.: HY-185446CAS No.: 1801756-14-8KZ-02 is an orally active dual MEK1/Pim-1 kinase inhibitor, with an IC50 of 1.07 nM against MEK1 and an IC50 of 1.34 μM against Pim-1. KZ-02 reduces the phosphorylation levels of ERK and Cdc25C, and promotes the proteasomal degradation of Pim-1 protein. KZ-02 inhibits cancer cell growth and exerts anti-tumor effects. KZ-02 can be used in the research of colorectal cancer.
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PIM1-IN-6
0 ImagesCat. No.: HY-147920CAS No.: 2439168-69-9PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor, with an IC50 of 0.60 μM. PIM1-IN-6 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 1.51 and 15.2 μM, respectively.
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FD2024
0 ImagesCat. No.: HY-181925FD2024 is a pan-PIM kinase inhibitor with IC50 values of 0.17 nM, 1.86 nM, and 0.38 nM against PIM-1, PIM-2, and PIM-3, respectively. FD2024 induces cell apoptosis. FD2024 inhibits the phosphorylation of mTOR, p70S6K, S6, 4EBP1, and BAD proteins. FD2024 exhibits anti-acute myeloid leukemia activity. FD2024 can be used in studies related to acute myeloid leukemia.
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PIM-1/HDAC-IN-2
0 ImagesCat. No.: HY-174302CAS No.: 3103925-33-0PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
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Multi-target kinase-IN-8
0 ImagesCat. No.: HY-179098Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf V600E (IC50 = 0.078 µg/mL), c-Met (IC50 = 0.405 µg/mL), Pim-1 (IC50 = 1.053 µg/mL), EGFR WT (IC50 = 0.177 µg/mL), VEGFR-2 (IC50 = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly used in cancer research.
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Pim-1 kinase inhibitor 3
0 ImagesCat. No.: HY-150731CAS No.: 2801695-39-4Pim-1 kinase inhibitor 3 (Compound H5) is a potent Pim-1 kinase inhibitor with an IC50 of 35.13 nM.
