2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis Bcl-2 Family Caspase
  4. CHNQD-01522

CHNQD-01522 is a microtubule inhibitor targeting the colchicine binding site on β-tubulin. CHNQD-01522 binds to the colchicine binding site on β-tubulin, inhibits microtubule polymerization, and evades P-glycoprotein transport in cancer cells. CHNQD-01522 inhibits proliferation, suppresses tumor cell colony formation, arrests cell cycle in G2/M phases, and induces apoptosis in cancer cells. CHNQD-01522 upregulates of Bax and activation of caspase-9 and caspase-3. CHNQD-01522 shows anti-tumor efficacy in subcutaneous and orthotopic hepatocellular carcinoma xenograft tumor models. CHNQD-01522 can be used for the research of hepatocellular carcinoma.

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CHNQD-01522

CHNQD-01522 Chemical Structure

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CHNQD-01522 Related Antibodies

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

CHNQD-01522 is a microtubule inhibitor targeting the colchicine binding site on β-tubulin. CHNQD-01522 binds to the colchicine binding site on β-tubulin, inhibits microtubule polymerization, and evades P-glycoprotein transport in cancer cells. CHNQD-01522 inhibits proliferation, suppresses tumor cell colony formation, arrests cell cycle in G2/M phases, and induces apoptosis in cancer cells. CHNQD-01522 upregulates of Bax and activation of caspase-9 and caspase-3. CHNQD-01522 shows anti-tumor efficacy in subcutaneous and orthotopic hepatocellular carcinoma xenograft tumor models. CHNQD-01522 can be used for the research of hepatocellular carcinoma[1].

IC50 & Target[1]

Bax

 

Caspase 3

 

Caspase-9

 

In Vitro

CHNQD-01522 (Compound 18) (72 h) potently inhibits proliferation of Huh-7, Hep G2, A549, HT-29, U251, and BT-549 cells with IC50 values of 0.17-0.3 μM, and exhibits favorable selectivity for cancer cells over normal L-02 liver cells[1].
CHNQD-01522 (0.125-0.25 μM; 5 days) dose-dependently inhibits colony formation of Huh-7 cells, with near-complete inhibition at 0.25 μM over 5 days[1].
CHNQD-01522 (0.125-0.25 μM; 24 h) induces G2/M phase cell cycle arrest in Huh-7 cells, with a marked increase in G2/M phase cells at 0.25 μM after 24 h[1].
CHNQD-01522 (0.125-0.25 μM; 24 h) induces significant apoptosis in Huh-7 cells, with a marked increase in total apoptotic cells at 0.25 μM after 24 h[1].
CHNQD-01522 (0.125-0.5 μM; 24 h) activates the mitochondrial intrinsic apoptotic pathway in Huh-7 cells via dose-dependent upregulation of Bax and activation of caspase-9 and caspase-3 after 24 h of treatment[1].
CHNQD-01522 (10-20 μM; 90 min) dose-dependently inhibits tubulin polymerization, acting as a microtubule-destabilizing agent[1].
CHNQD-01522 (0.125-0.25 μM; 6 h) disrupts the microtubule cytoskeleton organization in Huh-7 cells after 6 h of treatment at 0.125 μM and 0.25 μM[1].
CHNQD-01522 (10-100 μM; 1 h) directly interacts with β-tubulin in Huh-7 cell lysates, increasing its stability against proteolytic digestion[1].
CHNQD-01522 (10-100 μM; 2 h) competes with EBI for the colchicine binding site on β-tubulin in Huh-7 cells[1].
CHNQD-01522 is not a substrate of P-gp and does not modulate P-gp efflux function, indicating inherent resistance to P-gp-mediated multidrug resistance[1].

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

CHNQD-01522 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: Huh-7
Concentration: 0.125 μM, 0.25 μM
Incubation Time: 24 h
Result: Increased the proportion of G2/M phase-arrested cells.
Reduced the proportion of G1 phase-arrested cells.

Apoptosis Analysis[1]

Cell Line: Huh-7
Concentration: 0.125 μM, 0.25 μM
Incubation Time: 24 h
Result: Raised the total apoptotic cell population from 2.51% (control) to 31.84% at 0.25 μM.

Western Blot Analysis[1]

Cell Line: Huh-7
Concentration: 0.125 μM, 0.25 μM, 0.5 μM
Incubation Time: 24 h
Result: Upregulated Bax expression in a dose-dependent manner.
Activated caspase-9 and caspase-3 in a dose-dependent manner.

Immunofluorescence[1]

Cell Line: Huh-7
Concentration: 0.125 μM, 0.25 μM
Incubation Time: 6 h
Result: Induced marked disruption of the microtubule cytoskeleton, with structural alterations similar to those caused by vincristine.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t MRT0-t F C0
Rat[1] 2.5 mg/kg i.v. 0.336 h 0.083 h 6140.244 ng/mL 3180.121 ng·h/mL 0.356 h 100 % 7515.850 ng/mL
Rat[1] 10 mg/kg i.p. 1.326 h 0.083 h 12122.205 ng/mL 11041.089 ng·h/mL 1.097 h 86.8 % /
Rat[1] 30 mg/kg p.o. 8.421 h 0.25 h 822.671 ng/mL 3325.864 ng·h/mL 14.011 h 8.715 % /
In Vivo

CHNQD-01522 (Compound 18) (2 mg/kg; i.p.; QD/BID/TID; 14 days) demonstrates significant dose frequency-dependent anti-hepatocellular carcinoma activity in a Huh‑7 subcutaneous xenograft model, with a 79.09% tumor weight growth inhibition rate at the 2 mg/kg TID dosing schedule, and exhibits a favorable safety profile[1].
CHNQD-01522 (1 mg/kg; i.p.; three times daily (TID); 14 days) significantly reduces tumor volume in an Huh-7 orthotopic hepatocellular carcinoma xenograft model, with no observed body weight loss[1].

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

Animal Model: BALB/c-nu (female, 6-7 weeks old, 14 ± 1 g, Huh‑7 subcutaneous xenograft model)[1]
Dosage: 2 mg/kg
Administration: i.p.; QD/BID/TID; 14 days
Result: Achieved a tumor growth inhibition (TGI) rate of 70.22% for tumor volume and 79.09% for tumor weight with 2 mg/kg TID regimen.
Delayed tumor progression in a dosing frequency-dependent manner.
Caused no significant body weight changes or adverse effects in any treated groups.
Animal Model: BALB/c-nu (female, 6-7 weeks old, 14 ± 1 g, Huh‑7 orthotopic xenograft model)[1]
Dosage: 1 mg/kg
Administration: i.p.; TID; 14 days
Result: Resulted in a statistically significant reduction in tumor volume compared to the control group.
Caused no notable body weight changes in the treatment group.
Molecular Weight

354.36

Formula

C19H18N2O5
SMILES

COC1=CC(C(C(N2)=NC3=CC(C)=CC=C3C2=O)=O)=CC(OC)=C1OC
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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CHNQD-01522 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-01522CHNQD01522CHNQD 01522Microtubule/TubulinApoptosisBcl-2 FamilyCaspaseP-glycoproteinhepatocellular carcinoma cellsHuh-7apoptosismitochondrial intrinsic apoptotic pathwaycolchicine binding sitemicrotubule polymerizationβ-tubulinG2/M phasesHep G2Inhibitorinhibitorinhibit

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