pyrimidine-carboxamide

4-Amino-1-(2-b-C-methyl-b-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine-5-carboxamide is a Nucleoside Derivative - 7-Deaza-purine nucleoside; 2'-Modified nucleoside.

4-Amino-1-(3-deoxy-3-fluoro-b-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine-5-carboxamide is a useful organic compound for research related to life sciences and the catalog number is TNU0278.

4-Amino-1-(β-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide is a purine nucleoside analog with broad antitumor activity against indolent lymphoid malignancies. Its anticancer mechanisms involve inhibiting DNA synthesis and inducing apoptosis, among others [1].

Nucleoside Derivatives - 7-Deaza-purine nucleosides; Natural product; inhibitor of protein kinase C

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.

SPOP-IN-6b is an effective inhibitor of speckle-type POZ protein (SPOP) with an IC50 of 3.58 μM and can be used in stuides about the treatment of renal cancer.

Reverse transcriptase-IN-3, a pyrimidine-5-carboxamide derivative, functions as an inhibitor of HIV-1, demonstrating potent activity against both wild-type and mutant strains of HIV-1.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

Syk inhibitor II, a cell-permeable, ATP-competitive, pyrimidine-carboxamide compound, selectively and reversibly inhibits Syk (IC50 = 41 nM).

SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, functions as an inhibitor of Salt-inducible kinases (SIKs), which play a role in M1 M2 macrophage polarization linked to inflammation. By inhibiting SIK activity, this compound increases anti-inflammatory cytokine IL-10 and decreases pro-inflammatory cytokine IL-12, demonstrating significant anti-inflammatory efficacy in a DSS-induced colitis model [1].