2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. CHNQD-03301

CHNQD-03301 is an orally active hypoxia-inducible factor-1α (HIF-1α) inhibitor (IC50 = 10.97 nM). CHNQD-03301 promotes the proteasomal degradation of HIF-1α protein, leading to its significant suppression. CHNQD-03301 can reverse HIF accumulation-induced angiogenesis and mitigate the HIF-induced erythrocytosis phenotype in zebrafish models. CHNQD-03301 can be used for the study of colon cancer.

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CHNQD-03301

CHNQD-03301 Chemical Structure

CAS No. : 3104302-65-7

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CHNQD-03301 Related Antibodies

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Description

CHNQD-03301 is an orally active hypoxia-inducible factor-1α (HIF-1α) inhibitor (IC50 = 10.97 nM). CHNQD-03301 promotes the proteasomal degradation of HIF-1α protein, leading to its significant suppression. CHNQD-03301 can reverse HIF accumulation-induced angiogenesis and mitigate the HIF-induced erythrocytosis phenotype in zebrafish models. CHNQD-03301 can be used for the study of colon cancer[1].

IC50 & Target[1]

HIF-1α

10.97 nM (IC50)

In Vitro

CHNQD-03301 (Compound 20) (0.01-1.0 μM, 24 h) dose-dependently reduces HIF-1α protein levels and decreases the expression of downstream target proteins CA9, REDD1, and PDK1 in HCT116 cells, the mRNA expression levels of downstream genes such as CA9, VEGF, and REDD1 are also significantly reduced[1].
CHNQD-03301 (0.4-1.6 μM) significantly reduces EPO mRNA level, inhibiting the hypoxia-induced angiogenesis in HCT116 cells[1].
CHNQD03301 shows the IC50 values for HCT116 cells are 2.31 μM under normoxia and 0.83 μM under hypoxia[1].
CHNQD-03301 (0.4-1.6 μM) induces cell cycle arrest at the G2 phase under hypoxic conditions in HCT116 cells[1].
CHNQD-03301 (0.4-1.6 μM) has no significant effect on HCT116 cell proliferation but markedly inhibits the proliferation of von Hippel-Lindau (VHL)-deficient RCC4 cells[1].
CHNQD-03301 (1-4 μM, 7-14 days) dose-dependently inhibits spheroid formation in HCT116 cells[1].
CHNQD-03301 (0.4-2.0 μM, 24 h) significantly inhibits the migration ability of HCT116 cells under hypoxic conditions and VHL-deficient RCC4 cells[1].

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

CHNQD-03301 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116 cells, RCC4 cells
Concentration: 0.01 μM, 0.1 μM, 1.0 μM
Incubation Time: 24 h
Result: Dose-dependently reduced HIF-1α protein levels and decreased the expression of downstream target proteins (CA9, REDD1, PDK1) in HCT116 cells.
Reduced HIF-1α protein levels in HCT116 cells exogenously overexpressing HIF-1α.
Effectively reduced HIF-1α and CA9 protein levels in RCC4 cells (VHL-deficient).

Cell Migration Assay [1]

Cell Line: HCT116 cells (under hypoxic conditions), VHL-deficient RCC4 cells
Concentration: 0.4 μM, 0.8 μM, 1.6 μM
Incubation Time: 24 h
Result: Significantly inhibited the migration ability of HCT116 cells under hypoxic conditions and VHL-deficient RCC4 cells.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ Tmax Cmax T1/2 MRT0-t CL MRT0-∞ F
Rat 20 mg/kg i.p. 38027.7 ng·h/mL 42652.2 ng·h/mL 4.0 h 3380.9 ng/mL 9.6 h 13.2 h 468.9 mL/h/kg / /
Rat 20 mg/kg p.o. 35926.6 ng·h/mL 40869.9 ng·h/mL 4 h 2332.2 ng/mL 9.3 h / 489.3 mL/h/kg 14.1 h 94.5 %
In Vivo

CHNQD-03301 (Compound 20) (1 mg/kg, p.o., once daily, 13-19 days) significantly inhibits the growth of MB49 allograft tumor and HCT116 xenograft tumor mice without significant toxicity[1].
CHNQD-03301 (100 mg/kg, p.o., once) shows no acute toxicity at the 100 mg/kg dose in mice, and the maximum tolerated dose (MTD) was above 100 mg/kg, indicating a good safety profile[1].

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

Animal Model: A tumor model was established in female C57BL/6J (8-week-old) mice by subcutaneous injection of MB49 mouse bladder cancer cells (1×105 cells/mouse)[1].
Dosage: 1 mg/kg
Administration: P.o., once daily for 13 days
Result: Low-dose oral administration effectively inhibited MB49 tumor growth (TGI = 52.0%) and showed no significant change in mouse body weight.
Animal Model: A tumor model was also established in female C57BL/6J (8-week-old) mice by subcutaneous injection of HCT116 human colon cancer cells (2×106 cells/mouse)[1].
Dosage: 1 mg/kg
Administration: P.o., once daily for 19 days
Result: Low-dose oral administration effectively inhibited MB49 tumor growth (TGI = 51.0%) and showed no significant change in mouse body weight.
Animal Model: Healthy female ICR mice[1].
Dosage: 100 mg/kg
Administration: P.o., once
Result: None of the mice died within 7 days.
No apparent difference in blood biochemistry parameters, including ALT, AST, LDH, UREA, CREA, UA, and CK.
Hematoxylin and eosin (H&E) staining results presented no pathological changes in the collected tissues (hearts, livers, spleens, lungs, kidneys, and duodenum).
Molecular Weight

392.40

Formula

C23H20O6
CAS No.
SMILES

OC1=CC=C(C2=CC(OC)=C3C(OC4=CC(OC(C)(C)O5)=C5C=C34)=C2OC)C=C1
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Purity & Documentation
References
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CHNQD-03301 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:

CHNQD-033013104302-65-7CHNQD03301CHNQD 03301HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHHypoxia-Inducible Factor-1αHIF-1αBenzofuranoid p-terphenylsTumor HypoxiaHCT116 XenograftMB49 AllograftInhibitorinhibitorinhibit

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