A 196 - CAS 1982372-88-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C18H16Cl2N4
Molecular Weight:
359.25
COA:
Inquire
Targets:
Others
Description:
A 196 is a potent and selective inhibitor of SUV420H1/H2 (IC50 = 25 and 144 nM, respectively) with 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. It was shown to inhibit the di- and tri-methylation of H4K20me in multiple cell lines (IC50 < 1 μM).
Brife Description:
SUV420H1/H2 inhibitor
Purity:
≥98% by HPLC
Synonyms:
A-196; 6,7-Dichloro-N-cyclopentyl-4-(4-pyridinyl)-1-phthalazinamine
MSDS:
Inquire
InChIKey:
ABGOSOMRWSYAOB-UHFFFAOYSA-N
InChI:
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)
Canonical SMILES:
C1CCC(C1)NC2=NN=C(C3=CC(=C(C=C32)Cl)Cl)C4=CC=NC=C4
1.The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity.
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 Nat Chem Biol. 2017 Mar;13(3):317-324. doi: 10.1038/nchembio.2282. Epub 2017 Jan 23.
Protein lysine methyltransferases (PKMTs) regulate diverse physiological processes including transcription and the maintenance of genomic integrity. Genetic studies suggest that the PKMTs SUV420H1 and SUV420H2 facilitate proficient nonhomologous end-joining (NHEJ)-directed DNA repair by catalyzing the di- and trimethylation (me2 and me3, respectively) of lysine 20 on histone 4 (H4K20). Here we report the identification of A-196, a potent and selective inhibitor of SUV420H1 and SUV420H2. Biochemical and co-crystallization analyses demonstrate that A-196 is a substrate-competitive inhibitor of both SUV4-20 enzymes. In cells, A-196 induced a global decrease in H4K20me2 and H4K20me3 and a concomitant increase in H4K20me1. A-196 inhibited 53BP1 foci formation upon ionizing radiation and reduced NHEJ-mediated DNA-break repair but did not affect homology-directed repair. These results demonstrate the role of SUV4-20 enzymatic activity in H4K20 methylation and DNA repair. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Products


CAS 236395-14-5 Eslicarbazepine Acetate

Eslicarbazepine Acetate
(CAS: 236395-14-5)

Eslicarbazepine acetate, (BIA 2-093), is a promising antiepileptic drug structurally related to Carbamazepine and Oxcarbazepine.

CAS 4673-26-1 Diphenyleneiodonium chloride

Diphenyleneiodonium chloride
(CAS: 4673-26-1)

Diphenyleneiodonium chloride has been found to be a GPR3 agonist and also exhibit inhibition against NO synthase, NADG reductase and NADPH oxidase.

CAS 109-57-9 Allylthiourea

Allylthiourea
(CAS: 109-57-9)

Allylthiourea is a metabolic inhibitor that selective inhibits ammonia oxidation.

CAS 890819-86-0 ML 349

ML 349
(CAS: 890819-86-0)

ML 349 is a lysophospholipase 2 inhibitor with IC50 value of 144 nM.

CAS 344930-95-6 SSR 69071

SSR 69071
(CAS: 344930-95-6)

SSR 69071 is a potent and high affinity human leukocyte elastase (HLE) inhibitor (IC50 = 3.9 nM) that displays species-selectivity (Ki = 0.017, 1.70, 3.01, 58 a...

SR9011
(CAS: 1379686-29-9)

SR9011, a synthetic REV-ERB agonist, has been found to have probable effect against sleep disorders and metabolic diseases. IC50: 790 nM and 560 nM for Rev-ErbB...

CAS 1135237-88-5 Exherin trifluoroacetate

Exherin trifluoroacetate
(CAS: 1135237-88-5)

Exherin trifluoroacetate is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities, which selectively...

CAS 321915-72-4 Albitiazolium bromide

Albitiazolium bromide
(CAS: 321915-72-4)

Albitiazolium bromide is a choline analogue acts as a cholinergic receptor antagonists, inhibits choline transport into Plasmodium-infected erythrocytes, thus p...

Chemical Structure

CAS 1982372-88-2 A 196

Quick Inquiry

Verification code

Featured Items