2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Androgen Receptor Apoptosis
  4. SC428

SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1.

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SC428 Chemical Structure

SC428 Chemical Structure

CAS No. : 1898232-70-6

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Based on 1 publication(s) in Google Scholar

SC428 Related Antibodies

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Description

SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1[1].

In Vitro

SC428 (10 nM- 1 μM, 48 h), which inhibits AR-V7 (IC50is 0.42 μM) and ARv567es (IC50 is 1.31 μM) activity in 293T (PSA-Luc)[1].
SC428 (5 μM, 5 h) reverses DHT-induced thermal stabilization of AR-FL (EC50 is 0.31 μM) in LNCaP (CETSA), inhibits ligand-induced activation of AR in a concentration-dependent manner and is an antagonist of the F887 L mutant[1].
SC428 (1, 2.5 and 5 μM, 30 min) inhibits the proliferation of LNCaP (IC50is 1.39 μM), VCaP (IC50 is 1.01 μM), 22RV1 (IC50 is 1.13 μM) AR-positive cell line. The ability of anti-proliferation is weak in AR-negative cell line PC3 (IC50 is 6.49 μM)[1].
SC428 (5 μM, 5 h) attenuates transcription of AR-regulated genes in LNCaP-AR cells (ChIP experiments) , blocks AR-FL chromatin binding (confocal imaging experiments) , and reduces nuclear translocation[1].
SC428 (2.5, 5 μmol/L, 24 h) inhibits AR signaling in prostate cancer cells that overexpress AR-V7[1].
SC428 (0.5, 1, 2.5 and 5 μM, 24 h) has inhibitory effects on both LNCaP-ARV7 and LNCaP- wt cells (Enzalutamide (HY-70002)-resistant), inhibiting PSA and UBE2C at both protein and mRNA levels (WB and qPCR) [1].
SC428 (5 μM, 5 h) disrupts AR-V7 dimer (immunoprecipitation assay) and nuclear localization (confocal imaging technique) in 22RV1 cells[1].

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

SC428 Related Antibodies

Real Time qPCR[1]

Cell Line: LNCaP-AR
Concentration: 5 μmol/L
Incubation Time: 24 h
Result: Inhibited AR-FL transcription significantly and rogen-mediated mRNA expression.

Real Time qPCR[1]

Cell Line: 22Rv1
Concentration: 2.5 and 5 μmol/L
Incubation Time: 24 h
Result: 2.5 mmol/L SC428 reduced AR-regulated gene mRNA to 50% of controls, whereas 5 mmol/L SC428 further reduced it to 10% to 30% of controls. AR-V7-dependent Ar signaling was blocked in 22Rv1 cells.

Real Time qPCR[1]

Cell Line: LNCaP-AR-V7
Concentration: 0.5, 1, 2.5 and 5 μmol/L
Incubation Time: 24 h
Result: Inhibited the expression of PSA gene in LNCaP-AR-V7 cells and significantly decreased the mRNA level of AR-V7 specific gene UBE2C.

Western Blot Analysis[1]

Cell Line: LNCaP-AR-V7
Concentration: 0.5, 1, 2.5 and 5 μmol/L
Incubation Time: 24 h
Result: Inhibited PSA-Luc with equal potency in LNCaP-AR-V7 and LNCaP-ARWT cells.

Western Blot Analysis[1]

Cell Line: LNCaP-AR-V7，22Rv1
Concentration: 5 μmol/L
Incubation Time: 5 h
Result: Reduced AR-V7 homodimer.

Cell Proliferation Assay[1]

Cell Line: LNCaP, VCaP, 22Rv1, PC3
Concentration: 1, 2.5 and 5 μmol/L
Incubation Time: 30 min
Result: Inhibited the proliferation of three AR-positive cell lines, and the anti-proliferation effect of SC428 on the AR-negative cell line PC3 was 6-fold lower than that on the AR-positive cell line.

Cell Proliferation Assay[1]

Cell Line: LNCaP-AR
Concentration: 0.1 μM - 10 μM
Incubation Time: 30 h
Result: Overcame the ENZ-resistant AR signaling and cell proliferation driven by AR-V7.
In Vivo

SC428 (60 mg/kg; intraperitoneal injection; once daily; 18 days) inhibited AR-V7 tumor growth by inducing tumor cell apoptosis in mice[1].
SC428 (90 mg/kg; intraperitoneal injection; five times a week; 3 weeks) inhibited the growth of AR-V7 in mice[1].

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

Animal Model: 22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice[1].
Dosage: 60 mg/kg
Administration: Intraperitoneal injection (i.p.) ; daily route 5 days a week; 3 weeks
Result: Reduced the tumor growth by 50% , the mice did not lose weight, and the tumor PSA was reduced to undetectable levels.
Animal Model: 22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice. Male Nu/Nu mice were surgically castrated when the implanted 22Rv1 cells achieved an average tumor size of 200 mm3[1].
Dosage: 90 mg/kg
Administration: Intraperitoneal injection (i.p.); daily route 5 days a week; 3 weeks
Result: Inhibited the growth of prostate cancer with high expression of AR-V7.Good drug tolerance, no significant weight loss.
Molecular Weight

337.32

Formula

C15H10F3N3OS
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

N#CC1=CC=C(NC(N/C=C/C2=CC=CS2)=O)C=C1C(F)(F)F
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
Purity & Documentation
References
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SC428 Related Classifications

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    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:

SC4281898232-70-6SC 428SC-428Androgen ReceptorApoptosisAndrogen receptor inhibitorAR ligand-binding domain (LBD) Prostate cancerResistance mechanismsInhibitorinhibitorinhibit

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