2. PROTAC MAPK/ERK Pathway GPCR/G Protein Apoptosis
  3. PROTACs Ras p38 MAPK TNF Receptor
  4. ZJK-807

ZJK-807 is a highly effective and selective PROTAC degrader targeting KRASG12D (DC50 = 79.5 nM in AsPC-1 cells). ZJK-807 shows minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D), inducing mutant-specific cytotoxicity. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer. Yellow: KRASG12D ligand (HY-W087383); Green: E3 ligase CRBN ligand (HY-178507); Black: Linker (HY-178506).

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

ZJK-807

ZJK-807 Chemical Structure

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ZJK-807 Related Antibodies

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Description

ZJK-807 is a highly effective and selective PROTAC degrader targeting KRASG12D (DC50 = 79.5 nM in AsPC-1 cells). ZJK-807 shows minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D), inducing mutant-specific cytotoxicity. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer. Yellow: KRASG12D ligand (HY-W087383); Green: E3 ligase CRBN ligand (HY-178507); Black: Linker (HY-178506)[1].

In Vitro

ZJK-807 (Compound A11) (10 μM, 0.5-24 h) results in a time-dependent reduction in KRASG12D levels and a significant decrease in pERK levels, and can continue to degrade even after it has been removed in AsPC-1 cells[1].
ZJK-807 (1-3 μM, 12-16 h), at 1 μM for 16 hours, promotes the strong recruitment of HA-KRASG12D to CRBN E3 ligase in AsPC-1 cells, proving the formation of ternary complexes, and at 3 μM for 12 hours, it significantly enhances the polyubiquitination of KRASG12D in the same cell line[1].
ZJK-807 (0.1-3 μM, 24 h) induces significant, concentration-dependent degradation of KRAS protein in AsPC-1 (KRASG12D) cells, and shows no appreciable degradation of KRAS protein was observed in other KRAS mutant cell lines[1].
ZJK-807 (1.5-10000 nM, 24 h) exhibits potent and concentration-dependent degradation of KRASG12D with DC50 values of 79.5 nM (DMAX 92%) in AsPC-1 cells, 130.8 nM (DMAX 92%) in GP2D cells, and 313.8 nM (DMAX 70%) in AGS cells, while it does not induce concentration-dependent degradation of CK1α or GSPT1 in AsPC-1 and GP2D cells[1].
ZJK-807 (3 or 5 days) exhibits antiproliferative effects on KRASG12D mutant cell lines, with IC50 values of 219.6 nM in AsPC-1, 273.5 nM in AGS, and 1110 nM in GP2D cells, and shows no substantial antiproliferative activity was observed in cell lines with wild-type or other KRAS mutations or on the normal cell line HEK-293T[1].
ZJK-807 (0.01-10 μM, 24 h) can reduce KRASG12D protein levels in a concentration-dependent manner in AGS cells even in the presence of secondary mutations, and although its inhibitory efficacy is reduced, it still inhibits Ba/F3 cells carrying KRASG12D/95mut or KRASG12D/96mut [1].
ZJK-807 significantly alters the transcriptome with notable down-regulation and pathway enrichment in RAS/MAPK signaling[1].

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

ZJK-807 Related Antibodies

Western Blot Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 10 μM
Incubation Time: 0.5 h, 1 h, 2 h, 4 h, 8 h, 12 h, 24 h
Result: Resulted in a time-dependent reduction in KRASG12D levels and a significant decrease in pERK levels, observed as early as 2 h post-treatment, indicating sustained downregulation of the ERK pathway for up to 24 h in AsPC-1 cells.

Western Blot Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 3 μM
Incubation Time: 12 h
Result: KRASG12D degradation was significantly alleviated by the competitive binding of MRTX1133 (1 μM) and thalidomide (40 μM).
Pretreatment with the NEDD8-activating E1 enzyme inhibitor MLN4924 (1 μM) or the proteasome inhibitor MG132 (3 μM) for 4 h effectively attenuated the degradation of KRASG12D protein in AsPC-1 cells.

Western Blot Analysis[1]

Cell Line: AGS cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Reduced KRASG12D protein levels in a concentration-dependent manner, even in the presence of secondary mutations in AGS cells.
In Vivo

ZJK-807 (Compound A11) (30 mg/kg, s.c., once daily for 28 days) effectively inhibits KRASG12D-driven tumor growth in AsPC-1 xenograft mice in vivo and exerts its anti-tumor effect by degrading KRASG12D protein, while also exhibiting good tolerability[1].

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

Animal Model: 5.0 × 106 AsPC-1 cells suspended in 100 μL of PBS and Matrigel were subcutaneously implanted into the right flank of male BALB/c nude mice[1].
Dosage: 30 mg/kg
Administration: S.c., once daily for 28 days
Result: Tumor growth was significantly inhibited with a 47% reduction in tumor volume compared to the Vehicle group.
No significant decrease in body weight was observed.
The tumor weight was significantly lower than that in the Vehicle group.
KRASG12D protein expression level was significantly reduced.
Molecular Weight

906.98

Formula

C50H48F2N10O5
SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC(N4CC5(CCC(N(C6CN(C7=NC(N8C[C@@](N9)([H])CC[C@@]9([H])C8)=C(C=NC(C%10=C%11C(C#C)=C(F)C=CC%11=CC(O)=C%10)=C%12F)C%12=N7)C6)C)CC5)C4)=C3)=O
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Purity & Documentation
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ZJK-807 Related Classifications

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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.

Keywords:

ZJK-807ZJK807ZJK 807PROTACsRasp38 MAPKTNF ReceptorTumor Necrosis Factor ReceptorTNFRKRASG12DCRBNCereblonProtein DegradationTernary Complex FormationDrug ResistanceInhibitorinhibitorinhibit

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