2. Epigenetics
  3. Histone Methyltransferase
  4. PR5-LL-CM01

PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.

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

PR5-LL-CM01 Chemical Structure

PR5-LL-CM01 Chemical Structure

CAS No. : 1005307-86-7

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Based on 1 publication(s) in Google Scholar

PR5-LL-CM01 Related Antibodies

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Description

PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies[1].

In Vitro

PR5-LL-CM01 has a range of IC50 at 2-4 μM in PDAC cells (PANC1, MiaPaCa2 and AsPC1, and a range of IC50 at 10-11 μM in CRC cells (HT29, HCT116 and DLD1). PR5-LL-CM01 has higher efficacy to specifically inhibit cancer cells and demonstrated low toxicity in normal cells. PR5-LL-CM01 strongly inhibited colony forming ability in both PANC1 and HT29 cells[1].
PR5-LL-CM01 inhibits NF-κB activation and its target gene expression in PDAC and CRC cells[1].
PR5-LL-CM01 (0-15 μM) dramatically decreases TNFα and IL8 expression in both PANC1 and HT29 cells[1].

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

PR5-LL-CM01 Related Antibodies
In Vivo

PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect[1].

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

Animal Model: 6-8 weeks old Male NSG mice (bearing PANC1 or HT29 cells)[1]
Dosage: 20 mg/kg (drug stock dissolved in 1:1 Cremophor:ethanol solution)
Administration: Intraperitoneally 3 times per week; 32 days (PANC1 model); 10 days (HT29 model)
Result: Led to significant tumor inhibition in both PANC1 and HT29 xenografted mice. Did not visibly affect the mice body weight.
Molecular Weight

401.51

Formula

C23H27N7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC=C(NC2=C3C(N(C4=CC=CC=C4)N=C3)=NC(NCCN(C)C)=N2)C=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 11.11 mg/mL (27.67 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4906 mL 12.4530 mL 24.9060 mL
5 mM 0.4981 mL 2.4906 mL 4.9812 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4906 mL 12.4530 mL 24.9060 mL 62.2649 mL
5 mM 0.4981 mL 2.4906 mL 4.9812 mL 12.4530 mL
10 mM 0.2491 mL 1.2453 mL 2.4906 mL 6.2265 mL
15 mM 0.1660 mL 0.8302 mL 1.6604 mL 4.1510 mL
20 mM 0.1245 mL 0.6226 mL 1.2453 mL 3.1132 mL
25 mM 0.0996 mL 0.4981 mL 0.9962 mL 2.4906 mL
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PR5-LL-CM01 Related Classifications

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:

PR5-LL-CM011005307-86-7Histone MethyltransferaseargininemethyltransferaseHT29HCT116DLD1PDACCRCtumorInhibitorinhibitorinhibit

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