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104 Results for "

PIM-1

" in MedChemExpress (MCE) Product Catalog:

Products (104)

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ARV-825

37 Publications Verification

Cat. No.: HY-16954

CAS No.: 1818885-28-7

Target:

PROTACs Epigenetic Reader Domain c-Myc Polo-like Kinase (PLK) CDK JAK STAT Pim Bcl-2 Family PAK Wnt β-catenin Caspase PARP Apoptosis Reactive Oxygen Species (ROS)

Research Areas:

Neurological Disease Cancer

ARV-825 is a BET protein PROTAC degrader that recruits cereblon, and it targets BRD2, BRD3, and BRD4 for degradation via the ubiquitin-proteasome pathway. ARV-825 downregulates c-MYC, PLK1, MYCN, CDK4/6, JAK2, pSTAT3/5, PIM1, and Bcl-xL, upregulates p21 and p27, and modulates H3K27Ac-mediated transcription, the G2/M checkpoint, the Wnt/β-catenin pathway, and amino acid transport pathways. ARV-825 induces G1 phase cell cycle arrest, caspase 3/PARP-mediated apoptosis, DNA damage, and reactive oxygen species (ROS) production, reduces mitochondrial respiration, and simultaneously inhibits cell proliferation, clonogenic growth, and cell migration. ARV-825 is used in research on gastric cancer, leukemia, neuroblastoma, and cholangiocarcinoma ^[1] .

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Pim1/AAK1-IN-1

13 Cited Publications

Cat. No.: HY-10371

CAS No.: 1093222-27-5

Purity: 98.40%

Synonyms: LKB1/AAK1 dual inhibitor

Target:

Pim

Research Areas:

Cancer

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

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Phen-DC3 Trifluoromethanesulfonate

13 Cited Publications

Cat. No.: HY-15594A

CAS No.: 929895-45-4

Purity: 98.99%

Synonyms: Phen-DC3 Triflate

Target:

G-quadruplex α-synuclein RIP kinase

Research Areas:

Neurological Disease Inflammation/Immunology

Phen-DC3 Trifluoromethanesulfonate is a bisquinolinium G-quadruplex (G4) ligand. Phen-DC3 Trifluoromethanesulfonate selectively binds to and stabilizes the hybrid quadruplex-duplex hybrid (QDH) derived from the PIM1 promoter. Phen-DC3 Trifluoromethanesulfonate also binds to the c-myc promoter Pu24T G4 via extensive π-stacking, and induces polymerase stalling at α-synuclein DNA and RNA G4 sequences. Phen-DC3 Trifluoromethanesulfonate downregulates LPS (HY-D1056)-induced TNFRSF21, RIPK3 and p-MLKL in VECs, and ameliorates CLP-induced pulmonary vascular leakage in septic rats. Phen-DC3 Trifluoromethanesulfonate can be used in studies related to neurodegenerative diseases and sepsis-associated vascular injury ^[1] .

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SGI-1776 free base

12 Cited Publications

Cat. No.: HY-13287

CAS No.: 1025065-69-3

Purity: 99.35%

Target:

Pim Apoptosis FLT3 PPAR FASTK STAT Mitochondrial Metabolism DNA/RNA Synthesis Bcl-2 Family

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 ^[1] .

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