Cat. No.: HY-156110

IGF2BP1-IN-1

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Based on 1 Customer Validation

IGF2BP1-IN-1, a Cucurbitacin B (HY-N0416) derivative, is a potent IGF2BP1 inhibitor (K_D = 2.88 nM). IGF2BP1-IN-1 binds directly to IGF2BP1, thereby inducing tumor cell cycle arrest, increasing apoptosis, and reducing autophagy. IGF2BP1-IN-1 can be used in research on NSLSC, colon, breast, liver, ovarian, pancreatic, and cervical cancers.

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

Purity: 99.94%
CAS No.: 3029447-08-0
Formula: C₄₂H₅₂FN₃O₁₀
Molecular Weight:777.87

Storage:

-20°C, protect from light, stored under nitrogen

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

IGF2BP1-IN-1 Chemical Structure

CAS No.: 3029447-08-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Bcl-xL

Bcl-2

All Bcl-2 Family Isoforms :

All CDK Isoforms :

All PARP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.009 μM Compound: A11	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
A549	IC₅₀	5 nM Compound: A11	Antiproliferative activity against wild type human A549 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against wild type human A549 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
A549	IC₅₀	92 nM Compound: A11	Antiproliferative activity against human A549 cells with IGF2BP1 knockdown assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells with IGF2BP1 knockdown assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
BXPC-3	IC₅₀	0.018 μM Compound: A11	Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
CFPAC-1	IC₅₀	0.037 μM Compound: A11	Antiproliferative activity against human CFPAC-1 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human CFPAC-1 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
HCT-116	IC₅₀	0.034 μM Compound: A11	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
HeLa	IC₅₀	0.015 μM Compound: A11	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
HepG2	IC₅₀	0.08 μM Compound: A11	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
L02	IC₅₀	0.1 μM Compound: A11	Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
MCF7	IC₅₀	0.056 μM Compound: A11	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
MDA-MB-231	IC₅₀	0.049 μM Compound: A11	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
PANC-1	IC₅₀	0.088 μM Compound: A11	Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]
SK-OV-3	IC₅₀	0.054 μM Compound: A11	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 37681508]

In Vitro

IGF2BP1-IN-1 (compound A11) (72 h) exhibits potent and selective inhibition of cell proliferation in human non-small cell lung cancer cells (A549) (IC₅₀ = 0.009 μM; SI = 11.11). IGF2BP1-IN-1 significantly inhibits the proliferation of various cancer cell lines, including HCT-116 (IC₅₀ = 0.080 μM), MDA-MB-231 (IC₅₀ = 0.049 μM), MCF-7 (IC₅₀ = 0.056 μM), SK-OC-3 (IC₅₀ = 0.054 μM), HeLa (IC₅₀ = 0.015 μM), HepG-2 (IC₅₀ = 0.080 μM), BXPC-3 (IC₅₀ = 0.018 μM), PANC-1 (IC₅₀ = 0.088 μM), and CFPAC-1 (IC₅₀ = 0.037 μM). IGF2BP1-IN-1 shows weaker inhibitory activity against the L02 cell line (IC₅₀ = 0.100 μM)^[1].
IGF2BP1-IN-1 (0.1-0.5 μM; 48 h) significantly induces apoptosis in human non-small cell lung cancer cells (A549) in a dose-dependent manner. IGF2BP1-IN-1 significantly inhibits autophagy in human non-small cell lung cancer cells (A549) in a dose-dependent manner^[1].
IGF2BP1-IN-1 (0.1-0.5 μM; 24 h) induces cell cycle arrest at the G2/M phase in human non-small cell lung cancer cells (A549)^[1].
IGF2BP1-IN-1 (0.625-10 μM) binds directly and irreversibly to recombinant IGF2BP1 in vitro with extremely high affinity (K_D = 2.88 nM)^[1].
IGF2BP1-IN-1 (1 μM; 2 h) binds directly to endogenous IGF2BP1 and increases its thermal stability in human non-small cell lung cancer (A549) cells^[1].
IGF2BP1-IN-1 (0.1-1.0 μM; 48 h) dose-dependently inhibits the expression of the downstream protein c-MYC, anti-apoptotic proteins Bcl-2 and Bcl-xl, and cell cycle proteins CDK4 and Cyclin D1, while inducing PARP cleavage in human non-small cell lung cancer (A549) cells^[1].
The antiproliferative activity of IGF2BP1-IN-1 (72 h) is significantly reduced in human non-small cell lung cancer (A549) cells where IGF2BP1 expression has been knocked down via siRNA (IC₅₀ value increased from 0.005 μM to 0.092 μM)^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

A549 cells
Concentration:

0.1 μM, 0.2 μM, 0.5 μM
Incubation Time:

24 h
Result:

Led to a significant accumulation of A549 cells in the G2/M phase, inducing cell cycle arrest.

Apoptosis Analysis^[1]

Cell Line:

A549 cells
Concentration:

0.1 μM, 0.2 μM, 0.5 μM
Incubation Time:

48 h
Result:

Significantly and dose-dependently induced apoptosis in A549 cells, especially remarkably increasing the proportion of late apoptotic cells.

Cell Autophagy Assay^[1]

Cell Line:

A549 cells
Concentration:

0.1 μM, 0.2 μM, 0.5 μM
Incubation Time:

48 h
Result:

Significantly elevated the LC3II to LC3I ratio and dose-dependently increased the expression level of p62 protein without notably affecting Beclin-1 expression, indicating the blockade of the autophagic degradation phase.

Western Blot Analysis^[1]

Cell Line:

A549 cells
Concentration:

0.1 μM, 0.2 μM, 0.5 μM, 1 μM
Incubation Time:

48 h
Result:

Dose-dependently inhibited the expression of c-MYC, Bcl-2, Bcl-xl, CDK4, and Cyclin D1 proteins, and promoted the cleavage of PARP, without altering the total level of IGF2BP1 protein itself.

In Vivo

IGF2BP1-IN-1 (compound A11) (0.75 mg/kg; i.p.; once daily for 14 days) demonstrates excellent in vivo safety in normal female C57BL/6J mice, causing neither mortality nor significant body weight loss^[1].
IGF2BP1-IN-1 (0.5 mg/kg; i.p.; once daily for the first 6 days, followed by every other day; for 21-23 days) significantly inhibits tumor growth in a BALB/c male nude mouse xenograft model subcutaneously inoculated with A549 cells, without inducing significant changes in body weight or toxic side effects such as ascites. IGF2BP1-IN-1 significantly improves immunohistochemistry (IHC) and H&E staining scores and increased the expression level of the apoptosis-related marker TUNEL^[1].

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

Animal Model:

Naive female C57BL/6J mice, without tumor induction^[1]
Dosage:

0.75 mg/kg
Administration:

i.p., once daily, for 14 days
Result:

Demonstrated good biosafety, showing no induction of weight loss or mortality in mice.

Animal Model:

BALB/c nude mice (male, 14-17 g) were subcutaneously injected of 1 × 10⁷ A549 cells^[1]
Dosage:

0.5 mg/kg
Administration:

i.p., once daily for the first 6 days, followed by every other day; for 21-23 days
Result:

Extremely significantly suppressed the volumetric expansion and weight gain of the A549 xenograft tumors in nude mice.
Achieved a remarkably high tumor growth inhibition (TGI) rate of 80%.
Demonstrated good biosafety, showing no induction of weight loss in mice and no toxic side effects.
Markedly increased proportion of cells exhibiting nuclear pyknosis and vacuolation in the treated tumor tissues.
Downregulated the expression level of Ki-67, a marker reflecting cellular proliferative activity in the tumor tissues.
Elevated the positive expression level of TUNEL, an indicator of DNA fragmentation and cell apoptosis in the tumor tissues.

Chemical Information

CAS No. 3029447-08-0
Appearance Solid
Molecular Weight 777.87
Formula C₄₂H₅₂FN₃O₁₀
Color White to off-white
SMILES

C[C@]12[C@@]3([H])[C@]([C@@]4([H])C(C(C)(C([C@H](C4)OC(CN5C(N(C6=CC=C(C=C6)F)C=N5)=O)=O)=O)C)=CC3)(C(C[C@@]1([C@@]([C@@H](C2)O)([H])[C@@](C)(O)C(/C=C/C(C)(C)OC(C)=O)=O)C)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (128.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2856 mL

6.4278 mL

12.8556 mL

5 mM

0.2571 mL

1.2856 mL

2.5711 mL

10 mM

0.1286 mL

0.6428 mL

1.2856 mL

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, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Shang FF, et al. Discovery of Triazolyl Derivatives of Cucurbitacin B Targeting IGF2BP1 against Non-Small Cell Lung Cancer. J Med Chem. 2023 Sep 8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2856 mL	6.4278 mL	12.8556 mL	32.1390 mL
	5 mM	0.2571 mL	1.2856 mL	2.5711 mL	6.4278 mL
	10 mM	0.1286 mL	0.6428 mL	1.2856 mL	3.2139 mL
	15 mM	0.0857 mL	0.4285 mL	0.8570 mL	2.1426 mL
	20 mM	0.0643 mL	0.3214 mL	0.6428 mL	1.6070 mL
	25 mM	0.0514 mL	0.2571 mL	0.5142 mL	1.2856 mL
	30 mM	0.0429 mL	0.2143 mL	0.4285 mL	1.0713 mL
	40 mM	0.0321 mL	0.1607 mL	0.3214 mL	0.8035 mL
	50 mM	0.0257 mL	0.1286 mL	0.2571 mL	0.6428 mL
	60 mM	0.0214 mL	0.1071 mL	0.2143 mL	0.5357 mL
	80 mM	0.0161 mL	0.0803 mL	0.1607 mL	0.4017 mL
	100 mM	0.0129 mL	0.0643 mL	0.1286 mL	0.3214 mL

Keywords

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IGF2BP1-IN-1

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

All Bcl-2 Family Isoforms

All CDK Isoforms

All PARP Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

IGF2BP1-IN-1 Related Classifications

HY-156110 Related Classifications