2. Metabolic Enzyme/Protease
  3. PI5P4K
  4. 066ATZ

066ATZ is a PIP4K2A/2B inhibitor with human PIP4K2A Ki 100 nM and PIP4K2B Ki 800 nM. 066ATZ binds to ATP-binding sites of PIP4K2A and PIP4K2B to block lipid kinase activity. 066ATZ can be used for the research of non-small cell lung cancer.

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

066ATZ

066ATZ Chemical Structure

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066ATZ Related Antibodies

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Description

066ATZ is a PIP4K2A/2B inhibitor with human PIP4K2A Ki 100 nM and PIP4K2B Ki 800 nM. 066ATZ binds to ATP-binding sites of PIP4K2A and PIP4K2B to block lipid kinase activity. 066ATZ can be used for the research of non-small cell lung cancer[1].

In Vitro

066ATZ (0.03-20 μM;) potently and selectively inhibits recombinant PIP4K2A (Ki = 170 nM) and PIP4K2B (Ki = 870 nM) in vitro[1].
066ATZ (0.5 μM) demonstrates high selectivity against most human protein kinases, with only CK2a and CK2a2 showing significant inhibition[1].
066ATZ (20 μM; 3 days) does not affect the in vitro growth rate of H1975* NSCLC cells[1].
066ATZ (20 μM) reduces the growth-promoting activity of M2a-polarized THP-1 macrophages towards H1975 NSCLC cells in vitro[1].

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

066ATZ Related Antibodies

Cell Viability Assay[1]

Cell Line: H1975 NSCLC cells
Concentration: 20 μM
Incubation Time: 3 days
Result: Had no effect on the growth rate of cultured H1975 cells, with cell number fold-change matching that of DMSO-treated control cells.
In Vivo

066ATZ (100 mg/kg; i.p.; 5 times weekly for 36 days) significantly reduces NSCLC xenograft tumor growth in female R2G2 mice[1].
066ATZ (10-100 mg/kg; i.p.; single dose; 4 consecutive daily doses) is well tolerated at doses up to 100 mg/kg in female nude mice, and causes a transient blood glucose drop at doses of 30 mg/kg and higher[1].
066ATZ (10 mg/kg; i.p.; single dose) has a short in vivo half-life of ~0.5 h in male C57BL/6 mice[1].

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

Animal Model: Rag2/IL2RG double knockout (R2G2) (female, 7 weeks old, 1 × 107 H1975 cells was injected subcutaneously to establish a xenograft model)[1]
Dosage: 100 mg/kg
Administration: i.p.; 5 times per week for 36 days
Result: Reduced average tumor volume significantly compared to vehicle control on day 24 of treatment (p < 0.01).
Showed a small increase in CD31 staining in tumor tissues, indicating enhanced angiogenesis.
Animal Model: nude (female)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: i.p.; single dose; 4 consecutive daily doses (100 mg/kg only)
Result: Caused a transient 14% blood sugar drop 30 min after injection in the 30 mg/kg and 100 mg/kg groups, but not in the 10 mg/kg group.
Showed no difference in steady-state blood glucose after 4 consecutive daily doses of 100 mg/kg.
Did not affect body weight at a dose of 100 mg/kg.
Animal Model: C57BL/6 (male)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
Result: Reached a maximum plasma concentration (Cmax) of 2,484 ng/mL (~5.1 μM) after a single dose.
Had a half-life (t1/2) of ~0.5 h.
Molecular Weight

489.56

Formula

C22H23N11OS
SMILES

CN1C([C@H](N(C2=NC(NC3=CN=C(S3)C4=NNN=N4)=NC=C21)C5CCCC5)CC6=NC=CC=C6)=O
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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066ATZ Related Classifications

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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:

066ATZPI5P4KPIP4KH1975 NSCLC cellsNSCLCTHP-1 macrophagesR2G2 micenon-small cell lung cancerM2a macrophageCK2αPIP4K2APIP4K2BCK2α'Inhibitorinhibitorinhibit

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