2. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage Apoptosis
  3. Proton Pump DNA/RNA Synthesis Apoptosis
  4. TIP48/49-IN-1

TIP48/49-IN-1 is an orally active, specific RUVBL1/2 (TIP48/49) ATPase inhibitor with an IC50 of 59 nM against purified RUVBL1/2. TIP48/49-IN-1 inhibits the DNA replication process, leading to S-phase arrest. TIP48/49-IN-1 induces apoptosis. TIP48/49-IN-1 can be used for the research of non-small cell lung cancer (NSCLC) cells.

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

TIP48/49-IN-1

TIP48/49-IN-1 Chemical Structure

CAS No. : 1807337-58-1

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

TIP48/49-IN-1 Related Antibodies

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Description

TIP48/49-IN-1 is an orally active, specific RUVBL1/2 (TIP48/49) ATPase inhibitor with an IC50 of 59 nM against purified RUVBL1/2. TIP48/49-IN-1 inhibits the DNA replication process, leading to S-phase arrest. TIP48/49-IN-1 induces apoptosis. TIP48/49-IN-1 can be used for the research of non-small cell lung cancer (NSCLC) cells[1].

In Vitro

TIP48/49-IN-1 (Compound B) (100 nM; 3 days) depletes the PIKK family proteins ATM, ATR and DNA-PKCS in H2009 NSCLC cells[1].
TIP48/49-IN-1 (100 nM; 24 h) alters the transcriptome of H2009 and H596 non-small cell lung cancer (NSCLC) cells, and significantly downregulates DNA replication-related genes[1].
TIP48/49-IN-1 (100 nM; 12 h) enhances the binding of PAQosome components to RUVBL1 and impairs PAQosome maturation/dissociation in H2009 non-small cell lung cancer cells[1].
TIP48/49-IN-1 (100 nM; 48 h) induces S-phase arrest and subsequent apoptosis in sensitive non-small cell lung cancer (NSCLC) cell lines, including H2009[1].
TIP48/49-IN-1 (100 nM; 24 h) delays S-phase progression in synchronized H2009 non-small cell lung cancer cells[1].
TIP48/49-IN-1 (100 nM; 12-72 h) initially reduces the levels of ssDNA and chromatin-bound RPA2 in H2009 non-small cell lung cancer cells, and subsequently induces replication catastrophe at 48 h, accompanied by high levels of ssDNA and RPA hyperloading[1].
TIP48/49-IN-1 (100 nM; 6-12 h) accelerates the replication fork speed of H2009 non-small cell lung cancer (NSCLC) cells at 6 h post-treatment[1].
TIP48/49-IN-1 (100 nM; 12 h) increases POLE abundance at active replication forks in H2009 non-small cell lung cancer cells and reduces core histone abundance[1].
TIP48/49-IN-1 (25-50 nM; 3 days) radiosensitizes 8 NSCLC cell lines, but exerts no such effect on normal bronchial epithelial cells HBEC3KT or HBEC30KT[1].
TIP48/49-IN-1 (25 nM; 3 days) slows the DSB repair kinetics in H2009 non-small cell lung cancer cells, but exerts no such effect on HBEC3KT normal bronchial epithelial cells[1].
TIP48/49-IN-1 (150 nM; 3 days) inhibits ionizing radiation damage repair in organoids derived from 5 patients with primary non-small cell lung cancer[1].

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

TIP48/49-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: H2009 non-small cell lung cancer (NSCLC) cells
Concentration: 100 nM
Incubation Time: 3 days
Result: Depleted cellular levels of PIKK-family members DNA-PKCS (PRKDC), ATM, and ATR.

Cell Cycle Analysis[1]

Cell Line: Sensitive NSCLC cell lines including H2009
Concentration: 100 nM
Incubation Time: 48 h
Result: Induced S-phase arrest, followed by progression to apoptosis evidenced by a sub-G1 population.
Increased γH2AX (a marker of replication stress) and cleaved PARP1 (a marker of apoptosis) in H2009 cells as confirmed by immunoblotting.

Immunofluorescence[1]

Cell Line: H2009 NSCLC cells and HBEC3KT normal cells
Concentration: 25 nM
Incubation Time: 3 days pre-incubation plus continuous incubation during post-IR repair period
Result: Delayed the resolution of γH2AX and 53BP1 foci post-IR in H2009 cells, indicating impaired DSB repair.
Had no effect on DSB repair kinetics in HBEC3KT cells.
In Vivo

TIP48/49-IN-1 (Compound B) (175 mg/kg/day; p.o.; twice daily on treatment days; schedule: 4 days on, 9 days off, 3 days on, 7 days off, 3 days on) significantly inhibits H2009 NSCLC xenograft growth in female NOD.CB17-PrkdcSCID/J mice by depleting RUVBL1/2-dependent PIKK-family proteins[1].
TIP48/49-IN-1 (175 mg/kg/day; p.o.; twice daily on treatment days; schedule: 4 days on, 9 days off, 3 days on, 7 days off, 3 days on) inhibits H596 NSCLC xenograft growth in female NOD.CB17-PrkdcSCID/J mice by depleting RUVBL1/2-dependent PIKK-family proteins, with modest efficacy relative to H2009 tumors[1].
TIP48/49-IN-1 (125 mg/kg/day; p.o.; twice daily on treatment days; schedule: 4 days of treatment with 9 A.M. and 5 P.M. doses, plus 2 Gy IR at 12 P.M. on treatment days, with an additional 2 Gy IR on the fifth day) potentiates the antitumor efficacy of ionizing radiation in H1299 NSCLC xenografts without causing obvious toxicity in female nude mice[1].

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

Animal Model: NOD.CB17-PrkdcSCID/J (female, 10-12 weeks old, average weight ~21g, subcutaneous xenograft of H2009 NSCLC cells)[1]
Dosage: 175 mg/kg/day
Administration: p.o.; twice daily on treatment days; schedule: 4 days on, 9 days off, 3 days on, 7 days off, 3 days on
Result: Reduced tumor growth.
Depleted tumor levels of ATM, ATR, and DNA-PKCS proteins.
Decreased ATM-positive tumor cell nuclei.
Induced stressed and vacuolated nuclei in tumors by H&E staining.
Caused transient bodyweight loss with no marked changes in kidney, liver, spleen, or small intestine tissue architecture or morphology.
Animal Model: NOD.CB17-PrkdcSCID/J (female, 10-12 weeks old, average weight ~21g, subcutaneous xenograft of H596 NSCLC cells)[1]
Dosage: 175 mg/kg/day
Administration: p.o.; twice daily on treatment days; schedule: 4 days on, 9 days off, 3 days on, 7 days off, 3 days on
Result: Reduced tumor growth (with a smaller effect than in H2009 xenografts).
Depleted tumor levels of ATM, ATR, and DNA-PKCS proteins.
Animal Model: Crl:NU-Foxn1nu nude (female, 10-12 weeks old, average weight ~23g, subcutaneous xenograft of H1299 NSCLC cells)[1]
Dosage: 125 mg/kg/day
Administration: p.o.; twice daily on treatment days; schedule: 4 days of treatment with 9 A.M. and 5 P.M. doses, plus 2 Gy IR at 12 P.M. on treatment days, with an additional 2 Gy IR on the fifth day
Result: Showed no effect on tumor growth when administered alone.
Significantly potentiated IR-induced tumor growth inhibition when combined with ionizing radiation.
Caused no obvious toxicity, as measured by stable mouse bodyweight.
Reduced ATM protein levels in tumors.
Molecular Weight

536.02

Formula

C28H30ClN5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCOC(C=CC(Cl)=C1)=C1C2=NN=C([C@@H](CCC3)C[C@@H]3C(NC(C(N(C4=CC=CC=C4)N5C)=O)=C5C)=O)O2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (186.56 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8656 mL 9.3280 mL 18.6560 mL
5 mM 0.3731 mL 1.8656 mL 3.7312 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.75 mg/mL (7.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.75 mg/mL (7.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8656 mL 9.3280 mL 18.6560 mL 46.6400 mL
5 mM 0.3731 mL 1.8656 mL 3.7312 mL 9.3280 mL
10 mM 0.1866 mL 0.9328 mL 1.8656 mL 4.6640 mL
15 mM 0.1244 mL 0.6219 mL 1.2437 mL 3.1093 mL
20 mM 0.0933 mL 0.4664 mL 0.9328 mL 2.3320 mL
25 mM 0.0746 mL 0.3731 mL 0.7462 mL 1.8656 mL
30 mM 0.0622 mL 0.3109 mL 0.6219 mL 1.5547 mL
40 mM 0.0466 mL 0.2332 mL 0.4664 mL 1.1660 mL
50 mM 0.0373 mL 0.1866 mL 0.3731 mL 0.9328 mL
60 mM 0.0311 mL 0.1555 mL 0.3109 mL 0.7773 mL
80 mM 0.0233 mL 0.1166 mL 0.2332 mL 0.5830 mL
100 mM 0.0187 mL 0.0933 mL 0.1866 mL 0.4664 mL
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TIP48/49-IN-1 Related Classifications

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:

TIP48/49-IN-11807337-58-1Proton PumpDNA/RNA SynthesisApoptosisnon-small cell lung cancerH596 NSCLC cellsPIKK-family proteinspatient-derived explantsRUVBL1H2009 NSCLC cellsPAQosome complexnormal bronchial epithelial cellsRUVBL2NSCLC cellsInhibitorinhibitorinhibit

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