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Cat. No.: HY-151939

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BLM-IN-2

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BLM-IN-2 is a Bloom's Syndrome Protein (BLM) inhibitor with an IC₅₀ value of 0.8 μM. BLM-IN-2 effectively suppresses the proliferation, invasion, cell cycle arrest and apoptosis of CRC cells. BLM-IN-2 can be used for the reserarch of colorectal cancer (CRC).

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CAS No.: 3037604-86-4
Formule: C₃₃H₃₈BrFN₄O
Masse moléculaire:605.58

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BLM-IN-2 Chemical Structure

CAS No.: 3037604-86-4

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 0.8 μM (BLM)^[1]

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Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.6 μM Compound: 21	Inhibition of colony formation in human HCT-116 cells incubated for 10 days by crystal violet staining based assay Inhibition of colony formation in human HCT-116 cells incubated for 10 days by crystal violet staining based assay	[PMID: 36459756]
HCT-116	IC₅₀	1 μM Compound: 21	Inhibition of cell invasion in human HCT-116 cells incubated for 48 hrs by crystal violet staining based transwell assay Inhibition of cell invasion in human HCT-116 cells incubated for 48 hrs by crystal violet staining based transwell assay	[PMID: 36459756]
HCT-116	IC₅₀	1.9 μM Compound: 21	Antiproliferative activity against wild type human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by propidium iodide staining based high-content imaging analysis Antiproliferative activity against wild type human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by propidium iodide staining based high-content imaging analysis	[PMID: 36459756]
HCT-116	IC₅₀	2.8 μM Compound: 21	Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36459756]
NCM460	IC₅₀	15.6 μM Compound: 21	Cytotoxicity against human NCM460 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Cytotoxicity against human NCM460 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36459756]
RKO	IC₅₀	0.7 μM Compound: 21	Inhibition of colony formation in human RKO cells incubated for 10 days by crystal violet staining based assay Inhibition of colony formation in human RKO cells incubated for 10 days by crystal violet staining based assay	[PMID: 36459756]
RKO	IC₅₀	5.4 μM Compound: 21	Cytotoxicity against human RKO cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Cytotoxicity against human RKO cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36459756]
SW480	IC₅₀	0.6 μM Compound: 21	Inhibition of colony formation in human SW480 cells incubated for 10 days by crystal violet staining based assay Inhibition of colony formation in human SW480 cells incubated for 10 days by crystal violet staining based assay	[PMID: 36459756]
SW480	IC₅₀	2.2 μM Compound: 21	Cytotoxicity against human SW480 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Cytotoxicity against human SW480 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 36459756]

In Vitro

BLM-IN-2 (0-20 μM) has good inhibitory effect on BLM unwinding and binding DNA with IC₅₀ values of 0.8 μM and 2.3 μM, respectively^[1].
BLM-IN-2 exhibits the potent BLM-dependent cytotoxicity against the CRC cells but weak against normal cells^[1].
BLM-IN-2 (3 μM; 48 h) disrupts the HRR level while inhibiting BLM located on the DSB site and trigger DNA damage in the CRC cells^[1].
BLM-IN-2 (0-5 μM; 48 h) effectively suppresses the proliferation and invasion of CRC cells, along with cell cycle arrest and apoptosis^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HCT116 cells; HCT116, SW480 and RKO cells
Concentration:

0-5 μM; 0.5, 1, 2 μM
Incubation Time:

48 h; 10 days
Result:

Induced proliferation arrest.
Completely inhibited the growth of cancer cells at the concentration around 2 μM, had a good anti-CRC activity.

Apoptosis Analysis^[1]

Cell Line:

HCT116, SW480 and RKO cells
Concentration:

1 μM
Incubation Time:

48 h
Result:

Induced apoptosis and necrosis in HCT116, SW480 and RKO.

Cell Cycle Analysis^[1]

Cell Line:

HCT116, SW480 and RKO cells
Concentration:

4 μM
Incubation Time:

48 h
Result:

Changed the cell proportion of the S or G2/M phase in CRC cells, arrested the cell cycle at the S phase in HCT116 and SW480 and arrested the cell cycle of HCT116, SW480 and RKO at the G2/M phase.

Cell Invasion Assay^[1]

Cell Line:

HCT116 cells
Concentration:

0.25, 0.5, 1, 2, 4 μM
Incubation Time:

48 h
Result:

Obviously decreased the invasion in HCT116 cells with an IC₅₀ value of 1.0 μM and had inhibitory on CRC invasion.

Chemical Information

CAS No. 3037604-86-4
Appearance Solid
Masse moléculaire 605.58
Formule C₃₃H₃₈BrFN₄O
Color Light yellow to yellow
SMILES

CCN(CCCNC1=C(C=C2C(N(C(/C=C/C3=CC=C(C=C3)C(C)C)=NC2=C1)CC4=CC=C(C=C4)Br)=O)F)CC
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 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)
Instruction de manipulation (2659 KB)

Références

[1]. Jia-Li Tu, et al. Design, synthesis and evaluation of N3-substituted quinazolinone derivatives as potential Bloom's Syndrome protein (BLM) helicase inhibitor for sensitization treatment of colorectal cancer. Eur J Med Chem. 2022 Nov 21;246:114944. [Content Brief]

Calculators

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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.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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BLM-IN-2

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Colorectal Cancer Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

BLM-IN-2

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Colorectal Cancer Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

BLM-IN-2 Related Classifications

HY-151939 Related Classifications