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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
26 Results for "
PIM-IN-2
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "PIM-IN-2" in MCE Product Catalog:
12
12 Publications Verification
SGI-1776 free base is an orally active Pim kinase and FLT3 inhibitor with IC50 values of 7 nM, 363 nM, 69 nM, and 44 nM for Pim-1, Pim-2, Pim-3, and FLT3, respectively. SGI-1776 free base downregulates C/EBP-α, PPAR-γ, FAS, Leptin, and RANTES, and decreases STAT-3 phosphorylation. SGI-1776 free base induces Apoptosis, cell cycle arrest, mitochondrial depolarization, and reduces RNA synthesis, protein synthesis, and Mcl-1. SGI-1776 free base inhibits adipogenesis and lipid accumulation. SGI-1776 free base has anticancer activity against leukemia [2] .
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Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with Ki values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma [2] .
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TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM) .
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4 Cited Publications
Cat. No.: HY-18095A
CAS No.: 1353858-99-7
CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively .
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4 Cited Publications
Cat. No.: HY-18095B
CAS No.: 1353859-00-3
CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively .
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2 Cited Publications
Synonyms: 10-AcetylphenoxazINe
HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research .
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SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity .
M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM .
Cat. No.: HY-W412264
CAS No.: 6320-51-0
Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer .
HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research .
Research Areas:
HS56 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 .
Cat. No.: HY-115590
CAS No.: 1902983-63-4
JP-11646 is a pan-PIM inhibitor with increased potency against PIM2 (IC50 = 0.5 nM). JP11646 is freely reversible and ATP non-competitive. JP-11646 results in a decrease of PIM1, 2, and 3 mRNA. JP-11646 can effectively inhibit cell viability in small cell lung cancer (SCLC) and large cell neuroendocrine carcinomas of the lung (LCNEC). JP-11646 can cause a decrease in p-4EBP-1 protein, increasing the cleavage of caspases while decreasing caspase-3. JP-11646 induces apoptosis or necroptosis in cells. JP-11646 leads to reductions in MYC paralogs. JP-11646 can be used for the study of SCLC, LCNEC, human acute leukemia (AML), multiple myeloma (MM), and triple-negative breast cancer (TNBC) [2] .
Cat. No.: HY-122665A
Purity: 98.01%
HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research .
Cat. No.: HY-157404
CAS No.: 2918764-16-4
Pim-1/2 kinase inhibitor 2 (compound 5b) is a competitive PIM-1 and PIM-2 kinase inhibitor with IC50s of 1.31 μM and 0.67 μM, respectively. Pim-1/2 kinase inhibitor 2 shows in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines .
Cat. No.: HY-162059
CAS No.: 2918764-57-3
Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation .
Cat. No.: HY-155529
CAS No.: 1422456-47-0
FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice .
Cat. No.: HY-13287A
CAS No.: 1173928-26-1
Research Areas:
SGI-1776 is an orally active Pim kinase and FLT3 inhibitor with IC50 values of 7 nM, 363 nM, 69 nM, and 44 nM for Pim-1, Pim-2, Pim-3, and FLT3, respectively. SGI-1776 downregulates C/EBP-α, PPAR-γ, FAS, Leptin, and RANTES, and decreases STAT-3 phosphorylation. SGI-1776 induces Apoptosis, cell cycle arrest, mitochondrial depolarization, and reduces RNA synthesis, protein synthesis, and Mcl-1. SGI-1776 inhibits adipogenesis and lipid accumulation. SGI-1776 has anticancer activity against leukemia [2] .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
