2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. MS1-96

MS1-96 is an orally active PD-L1 (programmed death-ligand 1) degrader. MS1-96 effectively reduced PD-L1 protein levels across multiple colorectal cancer (CRC) cell lines. MS1-96 directly binds to PD-L1 (KD = 2.58 μM) and enhances the interaction between HIP1R and PD-L1, thereby altering the intracellular trafficking of PD-L1 within clathrin-coated vesicles. MS1-96 induces abnormal N-glycosylation of PD-L1, destabilizing the protein and hastening its lysosome-mediated degradation. MS1-96 can be used for the study of colorectal cancer.

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MS1-96

MS1-96 Chemical Structure

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MS1-96 Related Antibodies

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Description

MS1-96 is an orally active PD-L1 (programmed death-ligand 1) degrader. MS1-96 effectively reduced PD-L1 protein levels across multiple colorectal cancer (CRC) cell lines. MS1-96 directly binds to PD-L1 (KD = 2.58 μM) and enhances the interaction between HIP1R and PD-L1, thereby altering the intracellular trafficking of PD-L1 within clathrin-coated vesicles. MS1-96 induces abnormal N-glycosylation of PD-L1, destabilizing the protein and hastening its lysosome-mediated degradation. MS1-96 can be used for the study of colorectal cancer[1].

IC50 & Target

PD-L1

2.58 μM (Kd)

In Vitro

MS1-96 (10 μM, 48 h) significantly reduces PD-L1 protein levels in RKO cells but shows no reduction in PD-L1 mRNA levels in RKO cells[1].
MS1-96 (0-3 μM, 0-48 h) induces PD-L1 degradation in RKO cells in a time- and dose-dependent manner[1].
MS1-96 (1.5 μM, 24 h) reduces the level of PD-L1 on the surface of RKO and LoVo cells[1].
MS1-96 (1.5 μM, 24 h) disrupts the PD-1/PD-L1 interaction by downregulating PD-L1 in RKO and LoVo cells[1].
MS1-96 (1.5 μM, 24 h) enhances the killing effect of T cells on RKO cells and reduced the number of surviving cells[1].
MS1-96 (1.5 μM, 24 h) increases LDH release in RKO cells following co-culture with activated PBMCs, indicating enhanced cytotoxicity[1].
MS1-96 (1.5 μM, 0-12 h) promotes the degradation of PD-L1 in existing RKO cells, rather than inhibiting translation, thus reducing PD-L1 levels[1].
MS1-96 (1.5 μM) degrades PD-L1 in RKO cells via the lysosomal pathway, independent of proteasomes or autophagy[1].
MS1-96 induces aberrant N-glycosylation of PD-L1 at N35, N192, N200, and N219 sites in RKO cells[1].

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

MS1-96 Related Antibodies
In Vivo

MS1-96 (0-400 mg/kg, p.o., once daily for 10 days) effectively inhibits colorectal cancer tumor growth in MC38 cell xenograft mice by downregulating PD-L1 that was strictly dependent on CD8+ T cells, with a good safety profile[1].
MS1-96 (0-400 mg/kg, p.o., once daily for 9 days) fails to inhibit MC38 tumor growth in immunodeficient MC38 cell xenograft mice[1].

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

Animal Model: C57BL/6 mice (female, 5 weeks old) were subcutaneously inoculated with 8 × 105 MC38 colorectal cancer cells[1].
Dosage: 0 mg/kg, 100 mg/kg, 200 mg/kg, 400 mg/kg
Administration: P.o., once daily for 8, 10 days
Result: The drug significantly inhibited the growth of MC38 tumors in a dose-dependent manner.
Tumor volume and weight were significantly reduced.
No significant change in mouse body weight indicated good drug tolerance.
Western blot analysis showed a significant decrease in PD-L1 protein levels in tumor tissues.
Depletion of CD8+ T cells alone or simultaneous depletion of CD4+ and CD8+ T cells had no anti-tumor effect.
Depletion of CD4+ T cells alone did not affect the anti-tumor effect.
Animal Model: Immunodeficient nude mice (female, 4 weeks old) were subcutaneously inoculated with 8 × 105 MC38 colorectal cancer cells[1].
Dosage: 0 mg/kg, 200 mg/kg, 400 mg/kg
Administration: P.o., once daily for 9 days
Result: Failed to inhibit the growth of MC38 tumors.
Molecular Weight

375.50

Formula

C25H29NO2
SMILES

O=C(NC1=CC(CC[C@]2([H])[C@]3([H])CC[C@@]4(C)[C@@]2([H])CC[C@@H]4O)=C3C=C1)C5=CC=CC=C5
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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MS1-96 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:

MS1-96PD-1/PD-L1PD-1/Programmed death-ligand 1colorectal cancerantitumor immunityPD-L1lysosomal degradationHIP1RInhibitorinhibitorinhibit

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