1. Apoptosis Epigenetics
  2. Apoptosis Histone Methyltransferase
  3. PRMT5-IN-33

PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity.

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PRMT5-IN-33 Chemical Structure

PRMT5-IN-33 Chemical Structure

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Description

PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity[1].

IC50 & Target[1]

PRMT5

10.9 nM (IC50)

PRMT1

6.89 μM (IC50)

In Vitro

PRMT5-IN-33 inhibits proliferation of cells Z-138 and MOLM-13, with IC50s of 123.2 nM and 248.6 nM, respectively[1].
PRMT5-IN-33 decreases levels of arginine symmetrical dimethylation (sDMA) in a dose-dependent manner[1].

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

Western Blot Analysis[1]

Cell Line: Z-138 and MOLM-13
Concentration: 50-500 nM
Incubation Time: 48 h
Result: Inhibited expression of sDMA.
In Vivo

PRMT5-IN-33 (60-120 mg/kg, i.g.,twice a day for 13 days) inhibits the MOLM-13 xenograft tumor growth in a dose-dependent manner in BALB/c mice without a body weight loss[1].
PRMT5-IN-33 (p.o., 10 mg/kg, single dosage) reveals a pharmacokinetic profils in ICR mice[1]:
.
Pharmacokinetic Analysis of PRMT5-IN-33 in ICR mice[1]

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

route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-inf (ng·h/mL) T1/2 (h)
po 10 0.25 6870 6730 6760 1.17
Animal Model: MOLM-13 xenograft tumor in nude BALB/c mice[1]
Dosage: 60-120 mg/kg
Administration: intragastrical administration (i.g.), twice a day for 13 days
Result: Exhibited a tumor growth inhibition rate (TGI) of 33% (60 mg/kg) and 52% (120 mg/kg)
Molecular Weight

554.46

Formula

C25H24BrN5O3S

SMILES

BrC1=CC2=CC=C(C=C2N=C1N)CC[C@@H]3[C@H]([C@H]([C@@H](C3)NC4=C(C=NC=N4)C(C5=CSC=C5)=O)O)O

Shipping

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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PRMT5-IN-33 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.

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Product Name:
PRMT5-IN-33
Cat. No.:
HY-162230
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