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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
143 Results for "
PIM
" in MedChemExpress (MCE) Product Catalog:
Products (143)
143 Results for "PIM" in MCE Product Catalog:
37
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:
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 .
22
13
13 Cited Publications
Synonyms: LKB1/AAK1 dual inhibitor
Pim1/AAK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AAK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
12
12 Cited Publications
Synonyms: Phen-DC3 Triflate
Target:
Research Areas:
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 .
11
8
PIM447 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 .
8
PIM447 (LGH447) 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 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis .
7
Category:
Flavonoids Flavones Labiatae Cassia Phenols Polyphenols Plants Disease Research Fields Cancer
Target:
7
Category:
Flavonols Flavonoids Eriocaulon L. Phenols Polyphenols Plants Eriocaulaceae Disease Research Fields Inflammation/Immunology
Target:
6
4
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 .
4
4
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) .
4
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 .
4
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 .
3
3 Cited Publications
Target:
Research Areas:
HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders .
3
3 Cited Publications
Research Areas:
CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
3
3 Cited Publications
Research Areas:
CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
3
3 Cited Publications
Cat. No.: HY-15698B
CAS No.: 1781742-22-0
Research Areas:
CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
2
2 Cited Publications
Cat. No.: HY-16976
CAS No.: 1428569-85-0
GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma .
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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
