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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
25 Results for "
SIK1
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "SIK1" in MCE Product Catalog:
26
26 Publications Verification
Synonyms: SIK inhibitor 1
Target:
Research Areas:
HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.
9
9 Cited Publications
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YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM) [1].
5
5 Cited Publications
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ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity [1] .
3
3 Cited Publications
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YKL-06-061 is a potent, selective, second-generation salt-inducible kinase (SIK) inhibitor with IC50 values of 6.56 nM/1.77 nM/20.5 nM for SIK1/2/3, respectively [1].
2
2 Cited Publications
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YKL-06-062 is a second-generation salt-inducible kinase (SIK) inhibitor with an IC50 of 2.12 nM/1.40 nM/2.86 nM for SIK1, SIK2 and SIK3, respectively [1].
Cat. No.: HY-159657
CAS No.: 3033846-10-2
Research Areas:
PF-07899895 (Compound 34) is a SIK inhibitor, with IC50 values of 1.2 nM, 0.9 nM, and 1.8 nM against SIK1, SIK2, and SIK3, respectively. PF-07899895 modulates the anti-inflammatory cytokine IL-10 in immune cells. PF-07899895 is applicable to research related to inflammatory diseases [1] .
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MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively [1]. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells . MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
Target:
Salt-inducible Kinase (SIK) Discoidin Domain Receptor RIP kinase LIM Kinase (LIMK) MAP3K Bcr-Abl Src TGF-β Receptor
Research Areas:
GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases [1].
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MRIA9, a chemical probe, is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC50 values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively [1].
Cat. No.: HY-E70861
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SIK1 is a MAP4 kinase. The SIK1 MAP4K regulates cell proliferation and cell expansion. SIK1 phosphorylates BIK1 and stabilizes it in a kinase activity-dependent manner. SIK1 Recombinant Human Active Protein Kinase is a recombinant SIK1 protein that can be used to study SIK1-related functions [1].
Cat. No.: HY-RS12912
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Sik1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sik1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-RS12911
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SIK1 Human Pre-designed siRNA Set A contains three designed siRNAs for SIK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-161440
CAS No.: 3033846-29-3
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SIK-IN-1 (Compound 53) is an inhibitor for salt-inducible kinase (SIK), which inhibits SIK1, SIK2 and SIK3 with IC50s of 0.1, 0.4 and 1.5 nM, respectively. SIK-IN-1 inhibits the release of TNFa with IC50 of 0.5 nM, stimulates the LPS (HY-D1056) -induced IL-10 release with EC50 of 4 nM in human macrophages [1].
Cat. No.: HY-178014
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SIK1-IN-1 (Compound 27) is a selective Salt-inducible kinase 1 (SIK1) inhibitor with an IC50 of 0.7 nM for SIK1 over SIK2 and SIK3. SIK1-IN-1 has no cytotoxicity against HEK293 cells and PBMCs (maximum concentration of 30 μM). SIK1-IN-1 also has potent inhibitory activities for 392 kinases, in particular tyrosine kinases, such as FGR, HCK and LYN) [1].
Cat. No.: HY-RS12913
Research Areas:
Sik1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sik1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-173191
CAS No.: 2760404-50-8
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SK-124 is an orally active salt-inducible kinase (SIK) inhibitor with an IC50 of 230 nM against SIK1, 4.1 nM against SIK2, and 21 nM against SIK3, exhibiting excellent kinome selectivity [1] . SK-124 blocks SIK-mediated CRTC2 phosphorylation, promotes CRTC2 nuclear translocation, and regulates vitamin D metabolism by upregulating renal Cyp27b1 and downregulating Cyp24a1 [1] . SK-124 upregulates the expression of bone-related genes, increases serum Ca 2+, 1,25-vitamin D and intact FGF23 levels, and suppresses endogenous PTH levels [1] . SK-124 can be used in studies related to osteoporosis, male osteoporosis, and chronic kidney disease-mineral and bone disorder .
Cat. No.: HY-120877A
Purity: 98.70%
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(R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 [1] .
Cat. No.: HY-171591
CAS No.: 2810810-00-3
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SIK2-IN-4 (Compound 4) is a highly selective SIK1/2 inhibitor (IC50s 0.143 and 0.076 μM, respectively). SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3) by targeting SIK1/2, thereby regulating cAMP response element binding protein (CREB)-dependent transcriptional activity. SIK2-IN-4 inhibits the production of pro-inflammatory cytokines such as TNF (IC50: 0.11 µM), IL-12/23 p40 (IC50: 0.25 µM), and IL-23 (IC50: 0.47 µM), while inducing the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 can be used to study intestinal inflammation and other chronic inflammatory diseases [1].
Cat. No.: HY-171590
CAS No.: 2810809-10-8
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SIK2-IN-3 is an orally active SIK1/2 selective inhibitor (IC50: 0.128/0.084 μM). SIK2-IN-3 inhibits CRTC3 phosphorylation and myeloid cell pro-inflammatory cytokine production. SIK2-IN-3 ameliorates systemic and tissue inflammatory responses in a mouse anti-CD40 colitis model [1].
Cat. No.: HY-184862
CAS No.: 1613711-28-6
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SIK2-IN-5 is a SIK family kinase inhibitor, with IC50 values of 0.1-1 μM against SIK2 and SIK3, and an IC50 value of >1 μM against SIK1. SIK2-IN-5 inhibits the kinase activities of SIK1, SIK2 and SIK3. SIK2-IN-5 can be used in the research of ovarian cancer and breast cancer [1].
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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
