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Ly101-4B

Name: Ly101-4B
Brand: TargetMol
SKU: T218098
Rating: 4.5 (1 reviews)

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Ly101-4B is an apoptosis (apoptosis) inducer and multi-target inhibitor with antiproliferative, antitumor, and cytotoxic effects. It reduces HSF1 expression, inhibits microRNA-214 synthesis, and downregulates the expression of HSP27, HSP70, and HSP90. Additionally, Ly101-4B represses E2F-dependent transcriptional activity and downregulates its target genes. By decreasing DNA synthesis, inhibiting the cell cycle, and hindering the G1/S phase transition, Ly101-4B induces caspase3/7-mediated apoptosis without affecting RNA synthesis or causing necrosis. The compound demonstrates selectivity towards pancreatic ductal adenocarcinoma cells with varying genotypes and degrees of E2F dependency. Moreover, Ly101-4B is applicable in research related to epithelial ovarian cancer and pancreatic ductal adenocarcinoma.

Ly101-4B

Cas No. 1415728-94-7

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	10-14 weeks	10-14 weeks
50 mg	Inquiry	10-14 weeks	10-14 weeks

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	Ly101-4B is an apoptosis (apoptosis) inducer and multi-target inhibitor with antiproliferative, antitumor, and cytotoxic effects. It reduces HSF1 expression, inhibits microRNA-214 synthesis, and downregulates the expression of HSP27, HSP70, and HSP90. Additionally, Ly101-4B represses E2F-dependent transcriptional activity and downregulates its target genes. By decreasing DNA synthesis, inhibiting the cell cycle, and hindering the G1/S phase transition, Ly101-4B induces caspase3/7-mediated apoptosis without affecting RNA synthesis or causing necrosis. The compound demonstrates selectivity towards pancreatic ductal adenocarcinoma cells with varying genotypes and degrees of E2F dependency. Moreover, Ly101-4B is applicable in research related to epithelial ovarian cancer and pancreatic ductal adenocarcinoma.
In vitro	Ly101-4B, when administered at concentrations of 20-100 μM for 24-48 hours, inhibits the proliferation of cisplatin-resistant human epithelial ovarian cancer cells SKOV3, induces apoptosis, and downregulates the expression of HSF1, HSP27, HSP70, and HSP90. At 20-100 μM for 48 hours, it reduces the viability of primary pancreatic cancer cells with Nupr1 deficiency and Nupr1 wt; KIC, showing significant differential effects at 100 μM. In MiaPaCa2 cells, Ly101-4B at 1-25 μM for 12-72 hours inhibits E2F activity in E2F-dependent luciferase reporter assays, and at 25 μM for 12-72 hours, it decreases cell viability, induces caspase 3/7-mediated apoptosis, and inhibits DNA synthesis without affecting RNA synthesis or causing necrosis. Furthermore, Ly101-4B demonstrates greater efficacy in E2F high-expressing primary PDAC cells (CRCM93, CRCM08, CRCM17) compared to E2F low-expressing primary PDAC cells (CRCM10, CRCM12, CRCM110, CRCM92), with a lower 72-hour IC50 value of 19.4 μM versus 44.1 μM.
In vivo	Ly101-4B (100 mg/kg; intraperitoneal injection; twice weekly; over 4 weeks) significantly suppresses the in vivo growth of ovarian tumors in female nude mice (athymic mice) by downregulating HSF1 and miR-214, without adverse effects.

Chemical Properties

Molecular Weight	442.51
Formula	C₂₃H₃₀N₄O₅
Cas No.	1415728-94-7
Smiles	C(N)(=O)C=1N(N=C(C#CC2=CC=C(CCCCCCC)C=C2)N1)[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Related Tags: Ly101-4B in vivo | Ly101-4B in vitro | Ly101-4B formula | Ly101-4B molecular weight