MW 260.25 Da, Purity >98%. PDE inhibitor. Selective cytochrome P450IA2 inhibitor (IC50 = 2.4 μM). Methyl xanthine derivative. Shows an expanded duration of action compared to theophylline (ab142599) in vivo. Orally active.
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Key facts
- CAS number
- 80288-49-9
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 260.25 Da
- Molecular formula
- C12H12N4O3
- PubChem identifier
- 3433
- Nature
- Synthetic
Target data
Alternative names
ACLS, Aryl hydrocarbon hydroxylase, C-terminal cleavage product of 180 kDa, CP 12, CP1A2_HUMAN, CXXC-type zinc finger protein 7, CXXC7, CYP1A2, CYPIA2, Cytochrome P(3)450, Cytochrome P450 1A2, Cytochrome P450 4, Cytochrome P450 family 1 polypeptide 2, Cytochrome P450 family 1 subfamily A polypeptide 2, Cytochrome P450 subfamily I aromatic compound inducible polypeptide 2, Cytochrome P450-P3, DNA binding protein, DNA-binding factor KBF1, Dioxin inducable P3 450, GCPS, GLI Kruppel family member GLI 3, GLI Kruppel family member GLI3 (Greig cephalopolysyndactyly syndrome), GLI family zinc finger 3, GLI3 C-terminally truncated form, GLI3 form of 190 kDa, GLI3 form of 83 kDa, GLI3 full length protein, GLI3-190, GLI3-83, GLI3FL, GLI3_HUMAN, Glioma associated oncogene family zinc finger 3, HRX, HTRX1, Lysine N-methyltransferase 2A, MEN1_HUMAN, MLL cleavage product C180, MLL1, MLL1A, MLL1_HUMAN, Menin, Microsomal monooxygenase, Mll, Multiple Endocrine Adenomatosis 1, Multiple Endocrine Neoplasia 1, N-terminal cleavage product of 320 kDa, NFKB-p105, Nuclear factor NF kappa B, Oncogene GLI3, P(3)450, P3 450, P450 4, P450 P3, P450 form 4, P450(PA), PAP A, PAPB, PPD IV, Suppressor Candidate Gene 2, TRX 1, Transcriptional activator GLI3, Transcriptional repressor GLI3R, Trithorax-like protein, Wermer syndrome, Xenobiotic monooxygenase, ZES, Zinc finger protein GLI 3, Zinc finger protein HRX, Zollinger Ellison Syndrome, flavoprotein-linked monooxygenase, p180, p320
Recommended products
MW 260.25 Da, Purity >98%. PDE inhibitor. Selective cytochrome P450IA2 inhibitor (IC50 = 2.4 μM). Methyl xanthine derivative. Shows an expanded duration of action compared to theophylline (ab142599) in vivo. Orally active.
Key facts
- CAS number
- 80288-49-9
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 260.25 Da
- Molecular formula
- C12H12N4O3
- PubChem identifier
- 3433
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
- Biochemical name
- Furafylline
- Biological description
PDE inhibitor. Selective cytochrome P450IA2 inhibitor (IC50 = 2.4 μM). Methyl xanthine derivative. Shows an expanded duration of action compared to theophylline (ab142599) in vivo. Orally active.
- Canonical SMILES
- CC1=NC2=C(N1)C(=O)N(C(=O)N2CC3=CC=CO3)C
- InChI
- InChI=1S/C12H12N4O3/c1-7-13-9-10(14-7)16(6-8-4-3-5-19-8)12(18)15(2)11(9)17/h3-5H,6H2,1-2H3,(H,13,14)
- InChIKey
- KGQZGCIVHYLPBH-UHFFFAOYSA-N
- IUPAC name
- 3-(furan-2-ylmethyl)-1,8-dimethyl-7H-purine-2,6-dione
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- Ambient
- Appropriate long-term storage conditions
- Ambient
- Storage information
- The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
KMT2A also known as MLL acts as a histone methyltransferase. It plays an important role in chromatin modification and transcription regulation by methylating histone H3 on lysine 4. The KMT2A gene is located on chromosome 11q23 encoding a protein with a mass around 430 kDa. Expression occurs in various tissues but is particularly high in hematopoietic cells. The mechanistic activity of KMT2A requires binding to cofactors such as menin which serves as an adapter for transcriptional regulation.
- Biological function summary
Lysine methylation catalyzed by KMT2A influences gene expression and cellular differentiation. The KMT2A functions within a multi-protein complex involving menin and other cofactors including trithorax group proteins. It interacts with proteins to regulate genes important for maintaining stem cell pluripotency and hematopoiesis. The balance of KMT2A activity supports normal cell cycle progression and prevents aberrant cellular transformation.
- Pathways
KMT2A occupies an essential position in the regulation of the Wnt and Notch signaling pathways. Interaction with proteins involved in these pathways such as beta-catenin in the Wnt pathway highlights its role in controlling cell fate determination and proliferation. Crosstalk with signaling molecules supports the maintenance of cellular identity particularly in embryonic development and hematopoietic lineage specification.
- Associated diseases and disorders
KMT2A abnormalities contribute to acute leukemia including acute myeloid leukemia and acute lymphoblastic leukemia. Chromosomal translocations involving KMT2A result in fusion proteins that disrupt normal gene regulation. Fusion partners like AF4 can drive oncogenic transformation. Another implication involves disorders of differentiation where dysregulation of KMT2A activity contributes to disrupted hematopoietic stem cell function and aberrant lineage specification.
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1 product image
Chemical Structure - Furafylline, PDE inhibitor (ab146021)
2D chemical structure image of ab146021, Furafylline, PDE inhibitor
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