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.

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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

 

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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Purity & Documentation
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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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