2. Metabolic Enzyme/Protease Stem Cell/Wnt
  3. E1/E2/E3 Enzyme YAP
  4. DDO-4033

DDO-4033 is a SPOP inhibitor (IC50 = 16.9 μM, Kd = 15.1 μM). DDO-4033 impairs the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts SPOP recruitment to its substrate LATS1, inhibits its polyubiquitination and subsequent degradation, and upregulates LATS1 expression. DDO-4033 has promising antitumor activity and is promising for renal cell carcinoma research.

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DDO-4033 Chemical Structure

DDO-4033 Chemical Structure

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DDO-4033 Related Antibodies

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Description

DDO-4033 is a SPOP inhibitor (IC50 = 16.9 μM, Kd = 15.1 μM). DDO-4033 impairs the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts SPOP recruitment to its substrate LATS1, inhibits its polyubiquitination and subsequent degradation, and upregulates LATS1 expression. DDO-4033 has promising antitumor activity and is promising for renal cell carcinoma research[1].

In Vitro

DDO-4033 shows antiproliferative activity against 786-O, A498, A549, HK-2 cells, with IC50s of 1.1, 0.68, 19.96, 18.78 μM, respectively, but has weak antiproliferative activity against HepG2 cells, with an IC50 > 50 μM[1].
DDO-4033 (0-3 μM, 0-32 h) inhibits SPOP-mediated LATS1 ubiquitination and degradation, downregulates the mRNA level of CTGF and CYR61 genes in A498 cells[1].
DDO-4033 (0-5 μM, 24 h) inhibits the colony formation and impairs the cell migratory capacity in A498 cells[1].
DDO-4033 shows affinity for SPOP under MST, BLI, and ITC detection, with Kds of 15.1, 4.96, 4.94 μM, respectively[1].

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

DDO-4033 Related Antibodies

Western Blot Analysis[1]

Cell Line: A498 cells
Concentration: 0 μM, 0.12 μM, 0.25 μM, 0.5 μM, 1 μM
Incubation Time: 0 h, 1 h, 2 h, 4 h,8 h, 12 h, 16 h, 32 h
Result: Inhibited LATS1 ubiquitination, prolongs the half-life of LATS1, and accumulates LATS1.

Cell Migration Assay [1]

Cell Line: A498 cells
Concentration: 0 μM, 0.5 μM, 1 μM
Incubation Time: 24 h
Result: Inhibited the colony formation and impaired the cell migratory capacity.
In Vivo

DDO-4033 (10-50 mg/kg, intratumorally (i.t.) and peritumorally (PTI), once daily, 3 weeks) inhibits tumor growth, upregulates LATS1 and activates the Hippo pathway in A498-Luc xenograft BALB/c nude mice model[1].

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

Animal Model: A498-Luc (1 × 107 cells containing 25% Matrigel, s.c.) xenograft BALB/c nude mice (female, 18-20 g, 4-6 weeks of age) model[1]
Dosage: 10 mg/kg, 50 mg/kg
Administration: i.t. and PTI, once daily, 3 weeks
Result: Inhibited tumor growth, upregulated LATS1 and activated the Hippo pathway, was low in toxicity and did not change organ tissues.
Molecular Weight

406.39

Formula

C20H18N6O4
SMILES

C#CC1=C([N+]([O-])=O)C=C(C(NC2=CC(C)=NN2C(N3)=NC(CCC)=CC3=O)=O)C=C1
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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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DDO-4033 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:

DDO-4033DDO4033DDO 4033E1/E2/E3 EnzymeYAPE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseYes-associated proteinInhibitorRenal cell carcinomaA498 cellsBALB/c nude miceinhibitorinhibit

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