2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. PROTACs Ras
  4. MS243

MS243 is a potent KRASG12D PROTAC degrader with a DC50 of 4.2 nM. MS243 promotes the proximity between KRASG12D and the VHL E3 ubiquitin ligase, drives the ubiquitination and proteasomal degradation of KRASG12D, and inhibits the proliferation of cancer cells harboring KRASG12D. MS243 can be used in the research of KRASG12D-carrying cancers, such as colon cancer and pancreatic cancer.
(Pink: KRas G12D ligand (HY-181733); Blue: VHL ligand (HY-170348); Black: linker (HY-W895436)).

For research use only. We do not sell to patients.

MS243

MS243 Chemical Structure

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MS243 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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K-Ras H-Ras N-Ras Ras

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Description

MS243 is a potent KRASG12D PROTAC degrader with a DC50 of 4.2 nM. MS243 promotes the proximity between KRASG12D and the VHL E3 ubiquitin ligase, drives the ubiquitination and proteasomal degradation of KRASG12D, and inhibits the proliferation of cancer cells harboring KRASG12D. MS243 can be used in the research of KRASG12D-carrying cancers, such as colon cancer and pancreatic cancer[1]. (Pink: KRas G12D ligand (HY-181733); Blue: VHL ligand (HY-170348); Black: linker (HY-W895436)).

IC50 & Target[1]

KRas G12D

4.2 nM (DC50)

In Vitro

MS243 (0-10 μM; 7 d) inhibits the proliferation of GP2 and AsPC-1 cells, with GI50 values of 84 nM and 283 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MS243 Related Antibodies
Molecular Weight

1220.48

Formula

C66H79F2N13O6S
SMILES

FC(C=C1)=C(C#C)C(C1=CC(O)=C2)=C2C3=NC=C4C(N=C(OC[C@H]5N(CCC(NCCCCCCCCC6=CN([C@H](C(N7[C@H](C(N[C@@H](C)C8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O)C(C)(C)C)N=N6)=O)CCC5)N=C4N%10C[C@H]%11N[C@H](CC%11)C%10)=C3F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MS243 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS243MS 243MS-243PROTACsRasAsPC-1 cellsKRAS-G12D-harboring cancer cellskras-g12d-harboring cancerKRAS-G12DubiquitinationGP2d cellsPanc04.03 cellsVHL E3 ubiquitin ligaseproteasomal degradationInhibitorinhibitorinhibit

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