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LC-2 is a potent first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.
| Molecular Weight | 1132.78 |
| Formula | C59H71ClFN11O7S |
| CAS Number | 2502156-03-6 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Elena De Vita, et al. ACS Cent Sci. The Missing Link between (Un)dгυggаbΙе and Degradable KRAS
| Related PROTAC Products |
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CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). |
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Indisulam is a carbonic anhydrase inibitor and antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition. |
| dBET6
dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity. |
| A1874
A1874 is a BRD4-degrading PROTAC which inhibits many cancer cell lines proliferation, with DC50 of 32 nM (induce BRD4 degradation in cells). |
| MZ 1
MZ 1 is a PROTAC BRD4 degrader, with Kd values of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively. |
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Products are for research use only. Not for human use. We do not sell to patients.
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