WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H407272
CAS#: 1982372-88-2
Description: A-196 is the first potent and selective chemical probe for SUV420H1 and SUV420H2. The in vitro activity of A-196 includes inhibition of SUV420H1 with IC50 = 25 nM and SUV420H2 with IC50 = 144 nM for methylation of H4K20me and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cell assays, A-196 inhibits the di- and tri-methylation of H4K20me in multiple cell lines with IC50 < 1 µM.
Hodoodo Cat#: H407272
Name: A-196
CAS#: 1982372-88-2
Chemical Formula: C18H16Cl2N4
Exact Mass: 358.08
Molecular Weight: 359.254
Elemental Analysis: C, 60.18; H, 4.49; Cl, 19.74; N, 15.60
Synonym: A-196; A 196; A196.
IUPAC/Chemical Name: 6,7-dichloro-N-cyclopentyl-4-(pyridin-4-yl)phthalazin-1-amine
InChi Key: ABGOSOMRWSYAOB-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H16Cl2N4/c19-15-9-13-14(10-16(15)20)18(22-12-3-1-2-4-12)24-23-17(13)11-5-7-21-8-6-11/h5-10,12H,1-4H2,(H,22,24)
SMILES Code: ClC1=C(Cl)C=C(C(C2=CC=NC=C2)=NN=C3NC4CCCC4)C3=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Histone H4 lysine 20 methylation is emerging as a crucial modification to ensure genomic integrity both in the absence and presence of genotoxic stress. The majority of histone H4 methylation is detected in the lysine 20 (H4K20) and is evolutionarily conserved from yeast to human. Each methylation state results in distinct biology: dimethylated H4K20 (H4K20me2) is involved in DNA replication and DNA damage repair, and trimethylated H4K20 (H4K20me3) results in silenced heterochromatic regions . Loss of histone H4 lysine 20 trimethylation (H4K20me3) is characteristic of human cancer and a potential prognostic marker in many types of cancers.
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The following data is based on the product molecular weight 359.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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1: Bromberg KD, Mitchell TR, Upadhyay AK, Jakob CG, Jhala MA, Comess KM, Lasko LM, Li C, Tuzon CT, Dai Y, Li F, Eram MS, Nuber A, Soni NB, Manaves V, Algire MA, Sweis RF, Torrent M, Schotta G, Sun C, Michaelides MR, Shoemaker AR, Arrowsmith CH, Brown PJ, Santhakumar V, Martin A, Rice JC, Chiang GG, Vedadi M, Barsyte-Lovejoy D, Pappano WN. The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity. Nat Chem Biol. 2017 Mar;13(3):317-324. doi: 10.1038/nchembio.2282. Epub 2017 Jan 23. PMID: 28114273.
