| Identification | Back Directory | [Name]
2(3H)-Benzoxazolone, 6-[[4-(1H-indol-5-ylcarbonyl)-1-piperazinyl]sulfonyl]- | [CAS]
2567914-01-4 | [Synonyms]
TH1760
2(3H)-Benzoxazolone, 6-[[4-(1H-indol-5-ylcarbonyl)-1-piperazinyl]sulfonyl]- | [Molecular Formula]
C20H18N4O5S | [MOL File]
2567914-01-4.mol | [Molecular Weight]
426.45 |
| Chemical Properties | Back Directory | [density ]
1.534±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (>25 mg/ml) | [form ]
solid | [pka]
8.55±0.70(Predicted) | [color ]
Off-white | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | [SMILES]
O=S(C1=CC(O2)=C(C=C1)NC2=O)(N3CCN(CC3)C(C4=CC5=C(C=C4)NC=C5)=O)=O |
| Hazard Information | Back Directory | [Description]
TH1760 (2567914-01-4) is a potent inhibitor (IC50 = 25 nM dGTP hydrolysis; 57 nM 6-thio-dGTP hydrolysis) of the NUDIX hydrolase NUDT15, an important enzyme involved in the hydrolysis thiopurine chemotherapeutics.? It was selective against other human NUDIX proteins as well as a panel of 44 kinases and the Eurofins Cerep SafetyScreen44 panel.? It was active in AML cell lines HL-60 and NB4 as well as HCT116 3-6 colorectal carcinoma cells and 697 B-ALL cells. | [Uses]
TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine[1][2]. | [storage]
Store at -20°C | [References]
Zhang et al. (2020), Development of a chemical probe against NUDT15; Chem. Biol. 16 1120 |
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