PIM3
PIM3 encodes a serine/threonine Pim kinase that supports tumor-cell survival by phosphorylating Bad and blocking Bad-mediated apoptosis in pancreatic cancer cells[1]. Mechanistically, PIM3 links survival signaling to apoptosis control, because PIM3 silencing or kinase inactivation reduces proliferation and increases apoptosis in pancreatic, hepatoma, and colon cancer models[1][2][3]. In disease models, PIM3 promotes pancreatic tumor growth and neovascularization through increased pSTAT3^Tyr705^, pSurvivin^Thr34^, HGF, EGF, FGF-2, and VEGF[3]. Compared with related isoforms, PIM3 shows a distinct experimental role because PIM3, but not PIM1 or PIM2 knockdown, downregulates STAT3^Tyr705^ phosphorylation in prostate cancer cells[4]. For research applications, PIM kinase inhibition with SGI-1776 suppresses PDAC growth, alters cell-cycle behavior, and sensitizes pancreatic cancer cells to gemcitabine[5].
Références:
- [1]. Li YY, et al. Pim-3, a proto-oncogene with serine/threonine kinase activity, is aberrantly expressed in human pancreatic cancer and phosphorylates bad to block bad-mediated apoptosis in human pancreatic cancer cell lines. Cancer Res. 2006 Jul 1;66(13):6741-7. [Content Brief]
- [2]. Fujii C, et al. Aberrant expression of serine/threonine kinase Pim-3 in hepatocellular carcinoma development and its role in the proliferation of human hepatoma cell lines. Int J Cancer. 2005 Mar 20;114(2):209-18. [Content Brief]
- [3]. Liu B, et al. Pim-3 promotes human pancreatic cancer growth by regulating tumor vasculogenesis. Oncol Rep. 2014 Jun;31(6):2625-34. [Content Brief]
- [4]. Okui T, et al. Antitumor effect of temsirolimus against oral squamous cell carcinoma associated with bone destruction. Mol Cancer Ther. 2010 Nov;9(11):2960-9. [Content Brief]
- [5]. Xu D, et al. Inhibition of oncogenic Pim-3 kinase modulates transformed growth and chemosensitizes pancreatic cancer cells to gemcitabine. Cancer Biol Ther. 2013 Jun;14(6):492-501. [Content Brief]
All Product Categories
-
PIM3 Produits associés (18)
Produits associés (18)
- 1
-
PIM-447 dihydrochloride
0 ImagesSynonyms: LGH447 dihydrochloridePIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis.
-
Uzansertib phosphate
0 ImagesSynonyms: INCB053914 phosphate
-
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 .
-
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.
-
SGI-1776-VHL-02
0 ImagesCat. No.: HY-186146CAS No.: 3013618-84-0SGI-1776-VHL-02 is a stereoselective PIM PROTAC degrader. SGI-1776-VHL-02 promotes the ubiquitination and degradation of PIM1, PIM2 and PIM3. SGI-1776-VHL-02 downregulates c-myc protein levels, induces Apoptosis. SGI-1776-VHL-02 has anti-cancer activity against prostate cancer. SGI-1776-VHL-02 can be used in studies related to prostate cancer.
-
Uzansertib
0 ImagesSynonyms: INCB053914
-
PIM1-IN-1
0 ImagesPIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.
-
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.
-
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.
-
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.
-
PIM3-IN-1 hydrochloride
0 ImagesCat. No.: HY-163442A
-
Bufothionine
0 ImagesBufothionine is an alkaloid. Bufothionine can be isolated from Cinobufacini. Bufothionine induces mitochondria-mediated Apoptosis. Bufothionine significantly reduces serum IL-6 concentration, suppresses p-Stat3tyr705, p-Stat3ser727 and Jak2 expressions. Bufothionine upregulates Atg5, Atg7 and LC3Ⅱ expressions. Bufothionine induces Autophagy. Bufothionine suppresses PIM3 expression. Bufothionine relieves symptoms of H22-tumor-bearing mice and exerts anti-inflammation activity. Bufothionine exerts anti-cancer activities against gastric cancer.
- 1
