Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate
Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate Basic information
- Product Name:
- Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate
- Synonyms:
-
- 4-[2-(4,6-Dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl]-1-piperazinecarboxylic acid ethyl ester
- Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate
- YMU1
- Thymidylate Kinase Inhibitor, YMU1
- Thymidylate Kinase Inhibitor, YMU1 - CAS 902589-96-2 - Calbiochem
- 1-Piperazinecarboxylic acid, 4-[2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl]-, ethyl ester
- YMU 1,inhibit,YMU-1,YMU1,Thymidylate Kinase Inhibitor, YMU1,Inhibitor,Thymidylate Kinase Inhibitor, YMU-1
- CAS:
- 902589-96-2
- MF:
- C17H22N4O4S
- MW:
- 378.45
- Mol File:
- 902589-96-2.mol
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Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate Chemical Properties
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble1mg/mL, clear (warmed)
- form
- White solid
- color
- white to light brown
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Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate Usage And Synthesis
Uses
YMU1 is a potent, reversible, and ATP-competitive inhibitor of human Thymidylate kinase (TMPK).
Biological Activity
YMU1 is a cell-permeable and nontoxic inhibitor of hTMPK (thymidylate kinase) th at sensitizes tumor cells to doxorubicin in vitro and in vivo.
in vivo
YMU1 (5 mg/kg, intraperitoneal injection, three times a week, for 25 days) and doxorubicin co-administered to mice inhibits tumor growth[1].
YMU1 (3-10 mg/kg, intraperitoneal injection, once every two days, for 30 days) inhibits the growth of A549 xenograft tumors in mice[2].
| Animal Model: | HCT-116 p53-/- cell transplantation model in nude mice[1] |
| Dosage: | 5 mg/kg; 3 times a week; 25 days |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Showed that tumors grew significantly slower in mice treated with doxorubicin. |
| Animal Model: | A549 nude mouse transplantation model[2] |
| Dosage: | 3,10 mg/kg; once every two days; 30 days |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Reduced tumor volume and weight in a dose-dependent manner. |
IC 50
STAT3
Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylateSupplier
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