1346607-05-3
1346607-05-3 structure
- Name: GSK621
- Chemical Name: 6-chloro-5-[2'-hydroxy-3'-(methyloxy)-4-biphenylyl]-3-[3-(methyloxy)phenyl]-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione
- CAS Number: 1346607-05-3
- Molecular Formula: C26H20ClN3O5
- Molecular Weight: 489.907
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2017-01-10 01:21:49
- Modify Date: 2024-01-11 13:49:58
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GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation[1].
| Name | 6-chloro-5-[2'-hydroxy-3'-(methyloxy)-4-biphenylyl]-3-[3-(methyloxy)phenyl]-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione |
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| Synonyms |
1H-Pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione, 6-chloro-5-(2'-hydroxy-3'-methoxy[1,1'-biphenyl]-4-yl)-3-(3-methoxyphenyl)-
6-Chloro-5-(2'-hydroxy-3'-methoxy-4-biphenylyl)-3-(3-methoxyphenyl)-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione gsk621 |
| Description | GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation[1]. |
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| Related Catalog | |
| In Vitro | GSK621 (30 μM) induces AMPKα T172, ACC (S79) and ULK1 (S555) phosphorylation[1]. GSK621 (30 μM) induces autophagy and apoptosis[1]. GSK621 treatment also induces PERK phosphorylation, a marker of ER stress, in AML cells[1]. Cell Proliferation Assay[1] Cell Line: MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 AML cell lines.0-30 μM. Concentration: 0-30 μM. Incubation Time: 4 d. Result: IC50 values ranged from 13 to 30 μM. Reduced the proliferation of all 20 lines and increased apoptosis in 17 (85%) lines. Cell Autophagy Assay[1]. Cell Line: AML cell lines and primary AML samples. Concentration: 30 μM. Incubation Time: 24 h. Result: Induced the formation of numerous intracytoplasmic vacuoles including autophagosomes. |
| In Vivo | GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft[1]. Animal Model: MOLM-14 cells xenografted into nude mice[1]. Dosage: 30 mg/kg. Administration: IP twice daily. Result: Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily. |
| References |
| Density | 1.4±0.1 g/cm3 |
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| Molecular Formula | C26H20ClN3O5 |
| Molecular Weight | 489.907 |
| Exact Mass | 489.109161 |
| LogP | 4.04 |
| Index of Refraction | 1.674 |
| Storage condition | -20℃ |