2. JAK/STAT Signaling Stem Cell/Wnt Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. STAT PARP Apoptosis
  4. NSC-368262

NSC-368262 is a STAT3 inhibitor. NSC-368262 selectively alkylates and covalently modifies STAT3 Cys468 at the DNA-binding interface of STAT3, blocks the DNA-binding activity of STAT3, and inhibits the phosphorylation of STAT3. NSC-368262 blocks the accumulation of activated STAT3 in the nucleus of cancer cells, induces PARP cleavage and apoptosis in cells, and inhibits tumor growth in mouse models. NSC-368262 can be used in research related to breast cancer and cervical cancer.

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

NSC-368262

NSC-368262 Chemical Structure

CAS No. : 299421-08-2

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NSC-368262 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

NSC-368262 is a STAT3 inhibitor. NSC-368262 selectively alkylates and covalently modifies STAT3 Cys468 at the DNA-binding interface of STAT3, blocks the DNA-binding activity of STAT3, and inhibits the phosphorylation of STAT3. NSC-368262 blocks the accumulation of activated STAT3 in the nucleus of cancer cells, induces PARP cleavage and apoptosis in cells, and inhibits tumor growth in mouse models. NSC-368262 can be used in research related to breast cancer and cervical cancer[1][2].

IC50 & Target[1]

STAT3

 

Cellular Effect
Cell Line Type Value Description References
SK-MEL-5 IC50
10 μM
Compound: 81; C48
Inhibition of recombinant STAT3 (unknown origin) expressed in Escherichia coli BL21 (DE3) cells assessed as reduction in DNA binding activity with SK-MEL-5 nuclear extract incubated for 30 mins by electrophoretic mobility shift assay
Inhibition of recombinant STAT3 (unknown origin) expressed in Escherichia coli BL21 (DE3) cells assessed as reduction in DNA binding activity with SK-MEL-5 nuclear extract incubated for 30 mins by electrophoretic mobility shift assay
[PMID: 31810784]
In Vitro

NSC-368262 (C48) (0-500 μM; 30 min) selectively blocks the DNA-binding activity of activated Stat3 homodimers and Stat1/Stat3 heterodimers in nuclear extracts of IFN-γ-stimulated human melanoma Sk-Mel-5 cells, with corresponding IC50 values of 10-50 μM and 50-100 μM[1].
NSC-368262 (0-300 μM; 30 min) inhibits the DNA-binding activity of Stat3 in nuclear extracts of Sk-Mel-5 human melanoma cells only when it interacts with the Stat3 protein prior to Stat3 binding to DNA[1].
NSC-368262 (0-600 μM; 30 min) inhibits the DNA-binding activity of Stat3 via modifying Cys468, leading to alkylation modification of Stat3[1].
NSC-368262 (40 μM; 2 h) completely inhibits Oncostatin M-induced nuclear accumulation of Stat3-YFP in serum-starved MEF-Stat3-YFP mouse embryonic fibroblasts[1].
NSC-368262 (1-20 μM; 2 h) dose-dependently inhibits Stat3-mediated transcriptional activity in HeLa-Stat3-Luc human cervical cancer cells, with an IC50 of 3-10 μM[1].
NSC-368262 (1-20 μM; 48 h) induces apoptosis in human breast cancer cells MDA-MB-468 and MDA-MB-231 with constitutive Stat3 activity, with an IC50 of 10-20 μM after 48 h of treatment, but fails to induce apoptosis in human prostate cancer cells LNCaP lacking constitutive Stat3 activity[1].
NSC-368262 (1-20 μM; 48 h) inhibits the phosphorylation of Stat3Tyr705, blocks the expression of Mcl-1, and induces PARP cleavage (apoptosis) in human breast cancer MDA-MB-468 cells after 48 h of treatment; at a concentration of 20 μM, it completely inhibits the phosphorylation of Stat3 and the expression of Mcl-1[1].
NSC-368262 (0-50 μM) potently and selectively inhibits the DNA-binding activity of STAT3 in vitro with an IC50 of 10 μM, and suppresses STAT3-mediated transcriptional activity in HeLa cells[2].

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

NSC-368262 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-468 human breast cancer cells, MDA-MB-231 human breast cancer cells, LNCaP human prostate cancer cells
Concentration: 1, 3, 10, 20 μM
Incubation Time: 48 h
Result: Induced apoptosis in MDA-MB-468 and MDA-MB-231 cells with an IC50 of 10-20 μM.
Did not induce apoptosis in LNCaP cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 human breast cancer cells
Concentration: 1, 3, 10, 20 μM
Incubation Time: 48 h
Result: Reduced Stat3 Tyr705 phosphorylation at 10 μM.
Completely inhibited Stat3 Tyr705 phosphorylation at 20 μM.
Fully blocked expression of pro-survival Stat3 target gene Mcl-1 at 20 μM.
Induced cleavage of PARP (a marker of apoptosis) at 20 μM.
Did not significantly inhibit activation state of p44/p42 MAP kinases even at 20 μM.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-last Vss CL Tmax Bioavailability
Mice[1] 3 mg/kg i.v. 0.23 h 7.9 μM 1.4 μM·h 0.78 L/kg 70 mL/min/kg / /
Mice[1] 3 mg/kg p.o. / 0.16 μM 0.12 μM·h / / 0.25 h 8.4 %
In Vivo

NSC-368262 (200 mg/kg; i.p.; 5 days per week; 8 weeks) significantly inhibits the growth of MDA-MB-468 human breast cancer xenografts in athymic nude mice[1].
NSC-368262 (100-200 mg/kg; i.p.; 5 days per week; 2 weeks) significantly inhibits the growth of C3L5 mouse breast cancer xenografts in vivo in syngeneic mouse models[1].

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

Animal Model: athymic nude mice (6-week-old)[1]
Dosage: 200 mg/kg
Administration: i.p.; once daily, 5 days per week; 8 weeks
Result: Inhibited tumor growth significantly compared to vehicle-treated controls.
Caused no lethal toxicity or greater than 10% body weight loss.
Animal Model: C3H/HeJ mice (female, 7-9-week-old)[1]
Dosage: 100 mg/kg; 200 mg/kg
Administration: i.p.; once daily, 5 days per week; 2 cycles
Result: Inhibited tumor growth significantly compared to vehicle-treated controls at 200 mg/kg.
Showed no specific quantitative outcome data for the 100 mg/kg dose.
Molecular Weight

410.43

Formula

C22H22N2O6
CAS No.
SMILES

OC=1C=C2OCOC2=CC1C(NC3=NC=CC=C3)C4=CC(OC)=C(OC)C(OC)=C4
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Storage

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Purity & Documentation
References
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NSC-368262 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:

NSC-368262299421-08-2NSC368262NSC 368262STATPARPApoptosispoly ADP ribose polymerase STAT3 inhibitorSk-Mel-5 cellsmouse embryonic fibroblastsHeLa-Stat3-Luc human cervical cancer cellsMDA-MB-468 cellsMDA-MB-231 cellsHeLa cellsbreast cancercervical cancerInhibitorinhibitorinhibit

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