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SLMP53-2 1826116-38-4

SLMP53-2 1826116-38-4

CAS No.: 1826116-38-4

SLMP53-2 is a mutated p53 reactivator. SLMP53-2 restores the wild-type-like conformation and DNA-binding ability of mutp
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SLMP53-2 is a mutated p53 reactivator. SLMP53-2 restores the wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing the interaction of mutp53-Y220C with Hsp70, thereby reestablishing p53 transcriptional activity. SLMP53-2 induces cell cycle arrest, apoptosis, and endoplasmic reticulum (ER) stress. SLMP53-2 has anticancer effect.

Physicochemical Properties


CAS # 1826116-38-4
Appearance Typically exists as solid at room temperature
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro SLMP53-2 (3.12-50 μM; 48 h) inhibits HCC1419 and HuH-7 cell growth at IC50 values that are comparable. SLMP53-2 considerably reduces the growth inhibitory action of non-tumor HFF-1 cells (IC50 of 50 µM)[1]. HuH-7 cells in the G0/G1 phase undergo cell cycle arrest and apoptosis due to SLMP53-2 (14-28 μM; 48-72 h) [1]. On the formation of HuH-7 cell colonies, SLMP53-2 (0.9-14 μM; 14 days) exhibits a concentration-dependent growth inhibitory impact [1]. In HuH-7 cells, SLMP53-2 (28 μM; 24 h) raises the amounts of phosphorylated eIF2α, spliced XBP1 (sXBP1) mRNA, and XBP1 nuclear protein [1]. SLMP53-2 (14 μM; 16-48 h) downregulates survivin and VEGF while upregulating the protein levels of MDM2, p21, GADD45, BAX, and KILLER in HuH-7 cells. HuH-7 p53KO cells no longer exhibit this effect. [1]. HuH-7 cells are sensitized to sorafenib by LMP53-2 (1.5 μM) [1].
ln Vivo In nude mice bearing HuH-7 xenografts, SLMP53-2 (50 mg/kg; ip for five administrations) decreases tumor volume and weight without clearly harmful side effects [1].
Animal Protocol Animal/Disease Models: Female Swiss nude mice injected with HuH-7 cells[1]
Doses: 50 mg/kg
Route of Administration: Twice-weekly intraperitoneal (ip)injections for five administrations
Experimental Results: Displayed anti-tumor activity in HCC xenograft mouse models. demonstrated no significant variation of body weight throughout the experiment. No significant differences were observed between the weight of spleen, liver, heart, and kidneys.
References

[1]. SLMP53-2 Restores Wild-Type-Like Function to Mutant p53 through Hsp70: Promising Activity in Hepatocellular Carcinoma. Cancers (Basel). 2019 Aug 10;11(8):1151.

[2]. Mutant p53 reactivator SLMP53-2 hinders ultraviolet B radiation-induced skin carcinogenesis. Pharmacol Res. 2022 Jan;175:106026.


Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)