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- 规格参数
- 包装参数
Biochem/physiol Actions
Potent and selective ULK1 inhibitor that sensitizes cancer cells to nutrient stress by suppressing autophagy induction and autophagic flux.
ULK-101 is a potent and selective ULK1 inhibitor (ULK1/2 IC50 = 8.3/30 nM) that inhibits ULK1-dependent cellular Beclin 1 phosphorylation (pSer15 IC50 = 390 nM) with greater kinome selectivity (4 off-target hits using a 327-kinase panel) and potency than SBI-0206965 (IC50 = 38 nM/cell-free ULK1 kinase assay, 2.4 μM/cellular Beclion 1 pSer15). ULK-101 sensitizes cells to nutrient stress in U2OS (EC50 = 6.3 μM vs. 22.3 μM with full media) and in KRAS mutant lung cancer cultures (full media/nutrient withdrawal EC50 ratio >5) by suppressing autophagy induction and autophagic flux.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | FC(F)(F)[C@H](C1CC1)NC(C2=CC(C3=C4N(N=C3)C=C(C5=CC=C(C=C5)F)C=N4)=CS2)=O |
| InChI | 1S/C22H16F4N4OS/c23-16-5-3-12(4-6-16)15-8-27-20-17(9-28-30(20)10-15)14-7-18(32-11-14)21(31)29-19(13-1-2-13)22(24,25)26/h3-11,13,19H,1-2H2,(H,29,31)/t19-/m0/s1 |
| InChI key | PFZRXJIYAFANHP-IBGZPJMESA-N |
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¥ 2013.69
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¥ 1956.41
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¥ 4390.38
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¥ 1476.00
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