1. GPCR/G Protein
  2. GCGR
  3. ANT308

ANT308 is a vasoactive intestinal polypeptide (VIP receptor) antagonist. ANT308 significantly enhances the activation and proliferation of T cells. ANT308 inhibits the migration and metastasis, induces apoptosis of melanoma tumor cells by inhibiting VIP-VPAC2 signaling and reducing the expression of MCAM and N-cadherin. ANT308 can be used for the study of acute myeloid leukemia (AML) and uveal melanoma (UVM).

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ANT308

ANT308 Chemical Structure

CAS No. : 2871680-36-1

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Description

ANT308 is a vasoactive intestinal polypeptide (VIP receptor) antagonist. ANT308 significantly enhances the activation and proliferation of T cells. ANT308 inhibits the migration and metastasis, induces apoptosis of melanoma tumor cells by inhibiting VIP-VPAC2 signaling and reducing the expression of MCAM and N-cadherin. ANT308 can be used for the study of acute myeloid leukemia (AML) and uveal melanoma (UVM)[1][2].

In Vitro

ANT308 (1-10 μM, 48 h) significantly enhances CD69 and Ki67 expressions in CD4+ and CD8+ T cells[1].
ANT308 (0.1-10 μM, 72 h) reduces the viability of B16F10 and HT-144 cells dose-dependently[2].
ANT308 (10 μM, 72 h) decreases the proportion of cells in S phase, and induces apoptosis in B16LS9 and Mel 290 cells[2].
ANT308 (10 μM, 8 h) significantly inhibits cell migration in the B16LS9, Mel290, and HT-144 cell lines[2].
ANT308 (72 h) reduces MCAM and N-cadherin expression by inhibiting VIP-VPAC2 signaling[2].

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

Cell Viability Assay[2]

Cell Line: B16F10 and HT-144 cells
Concentration: 0.1, 1, 5 and 10 μM
Incubation Time: 72 h
Result: Decreased the numbers of viable B16F10 and HT-144 cells by around 46 % and 27 %, respectively, compared to control cultures with 5 μM twice daily.

Apoptosis Analysis[2]

Cell Line: B16LS9 and Mel 290 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Increased percentages of apoptotic cells.

Cell Cycle Analysis[2]

Cell Line: B16LS9 and Mel 290 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Decreased cells in the S phase.

Cell Migration Assay [2]

Cell Line: B16LS9, B16F10, Mel 290 cells, HT-144 cells
Concentration: 10 μM
Incubation Time: 8 h
Result: Significantly inhibited cell migration in the B16LS9, Mel290, and HT-144 cell lines
In Vivo

ANT308 (6 nmol, s.c., once daily for 10-14 days) significantly prolongs the survival period of mice and reduce the tumor burden in AML model[1].
ANT308 (100 μg/100 μL PBS, s.c., twice a day for 10 days) reduces the number and size of liver metastases of mice following intraocular or subcutaneous melanoma injection, and shows a trend toward reducing tumor volume at the primary tumor site[2].

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

Animal Model: P815 cells induced AML model established in DBA/2j (H2Kd) mice[1]
Dosage: 6 nmol
Administration: Subcutaneous injection (s.c.), once daily for 10-14 weeks
Result: Significantly prolonged the survival period of mice and reduced the tumor burden.
Animal Model: B16LS9 induced UVM model and B16LS9 or B16LS9 induced subcutaneous melanoma model established in female C57BL6/J mice (8-10 weeks) and NRG (NOD Rag gamma) mice (10-11 months old)[2]
Dosage: 100 μg/100 μL PBS
Administration: Subcutaneous injection (s.c.), twice a day for 10 days
Result: Significantly reduced the number of liver metastases.
Reduced MCAM, but had no significant effect on N-cadherin expression.
had no significant effect on subcutaneous tumor volume.
Molecular Weight

3467.10

Formula

C156H261N47O40S

CAS No.
Sequence

Lys-Pro-Arg-Arg-Pro-Tyr-Thr-Ser-Asp-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Leu-Ile-Leu-Asn

Sequence Shortening

KPRRPYTSDYTRLRKQMAVKKYLNLILN

SMILES

O=C(N1[C@@H](CCC1)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N2[C@@H](CCC2)C(N[C@@H](CC3=CC=C(C=C3)O)C(N[C@@H]([C@H](O)C)C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(N[C@@H](CC4=CC=C(C=C4)O)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCSC)C(N[C@@H](C)C(N[C@@H](C(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CC5=CC=C(C=C5)O)C(N[C@@H](CC(C)C)C(N[C@@H](CC(N)=O)C(N[C@@H](CC(C)C)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC(C)C)C(N[C@@H](CC(N)=O)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCCCN)N

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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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  • 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.

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ANT308
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