2. Cell Cycle/DNA Damage Apoptosis MAPK/ERK Pathway GPCR/G Protein
  3. G-quadruplex Bcl-2 Family c-Myc Ras
  4. NSC 373981

NSC 373981 is a CARD11 G4 stabilizer. NSC 373981 stabilizes the CARD11 G4 structure and inhibits CARD11 transcription in cells. NSC 373981 also inhibits BCL2 and MYC. NSC 373981 suppresses the transcription of KRAS and TERT. NSC 373981 exhibits anticancer activity against diffuse large B-cell lymphoma.

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NSC 373981

NSC 373981 Chemical Structure

CAS No. : 95455-02-0

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NSC 373981 Related Antibodies

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Description

NSC 373981 is a CARD11 G4 stabilizer. NSC 373981 stabilizes the CARD11 G4 structure and inhibits CARD11 transcription in cells. NSC 373981 also inhibits BCL2 and MYC. NSC 373981 suppresses the transcription of KRAS and TERT. NSC 373981 exhibits anticancer activity against diffuse large B-cell lymphoma[1][2].

IC50 & Target[1]

BCL2

 

K-RAS

 

In Vitro

NSC 373981 (24 h; 37°C) exhibits stability across acidic, neutral, and basic conditions, and in human and mouse plasma following 24-hour incubation at 37°C[1].
NSC 373981 (2.5-10.0 µM; 24 h) represses CARD11, BCL2, and MYC mRNA expression in a dose-dependent manner in RIVA, HBL1, and HT DLBCL cells, with additional effects on KRAS and TERT in RIVA and HT cells, but has no effect on CARD11 expression in VAL DLBCL or GM22671 benign B cells[2].
NSC 373981 (0.02-40 µM; 72 h) exhibits low micromolar cytotoxicity in RIVA, HT, and GM22671 cells, with higher cytotoxicity in cells where it represses multiple oncogene mRNA levels, and cytotoxicity does not correlate with basal CARD11 expression[2].

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

NSC 373981 Related Antibodies

Real Time qPCR[2]

Cell Line: ABC DLBCL (RIVA, HBL1), GCB DLBCL (HT, VAL), benign GC B (GM22671) cells
Concentration: 2.5, 5.0, 10.0 µM
Incubation Time: 24 h
Result: Caused a significant, dose-dependent repression of CARD11 mRNA levels (45-90% reduction at 10 µM) in RIVA, HBL1, and HT cells.
Induced concurrent dose-dependent decreases in BCL2 and MYC mRNA levels in RIVA, HBL1, and HT cells.
Reduced KRAS mRNA by 25-30% in RIVA cells and TERT mRNA by 40-55% in HT cells at 10 µM.
Showed no significant change in CARD11 mRNA levels in VAL and GM22671 cells.
Reduced MYC mRNA in GM22671 cells at 10 µM.
In Vivo

NSC 373981 (37.5-150 mg/kg; i.v., i.p.; single dose) exhibits distinct pharmacokinetic profiles with a 58% i.p. bioavailability in male athymic nu/nu mice, with detectable Phase I and Phase II metabolites across multiple bodily fluids[1].

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

Animal Model: athymic nu/nu (male)[1]
Dosage: 37.5 mg/kg (i.v.); 150 mg/kg (i.p.)
Administration: i.v.; single dose; i.p.; single dose
Result: Achieved peak plasma concentration >5.9 μg/mL, terminal elimination half-life 1.2 hours, volume of distribution 694 mL, and plasma clearance 390 mL/hr following i.v. administration.
Reached peak plasma concentration 2.1 μg/mL at 15 minutes, terminal elimination half-life 36.8 hours, and 58% bioavailability following i.p. administration.
Detected multiple Phase I and Phase II metabolites in plasma, urine, feces, and bile, including those from aromatic nitro group reduction, primary alcohol moiety oxidation, benzylic hydroxylation, naphthalene moiety hydroxylation/dihydrodiol formation, and Phase II conjugation reactions.
Molecular Weight

257.24

Formula

C14H11NO4
CAS No.
SMILES

OCCC1=C([N+]([O-])=O)OC2=CC=C3C=CC=CC3=C21
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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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NSC 373981 Related Classifications

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  • 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 37398195455-02-0NSC373981NSC-373981G-quadruplexBcl-2 Familyc-MycRasMycTERTdiffuse large B cell lymphomaHT DLBCL cellsHBL1 cellsKRASBCL2CARD11MYCRIVA cellsbenign germinal center B cellsInhibitorinhibitorinhibit

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