Clofazimine
Based on 13 publication(s) in Google Scholar
Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.79%
- No. CAS: 2030-63-9
- Fòrmula: C27H22Cl2N4
- Peso molecular:473.40
-
Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Clofazimine
More- Sci Adv. 2025 Mar 21;11(12):eads9182. [Abstract]
- Commun Biol. 2025 Oct 6;8(1):1425. [Abstract]
- Antiviral Res. 2022 Aug:204:105365. [Abstract]
- Antimicrob Agents Chemother. 2025 May 23:e0024925. [Abstract]
- Antimicrob Agents Chemother. 2024 Oct 29:e0094524. [Abstract]
- Antimicrob Agents Chemother. 2023 Feb 16;67(2):e0145922. [Abstract]
- Microbiol Spectr. 2021 Sep 3;9(1):e0004521. [Abstract]
- Pathogens. 2025 Mar 21;14(4):302. [Abstract]
- PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]
- chemRxiv. 2026 Apr 6.
- Patent. US20250312336A1.
- Authorea. 2025 Sep 17.
- bioRxiv. 2023 Sep 17:2023.09.15.557802. [Abstract]
Customer Validation & Images
-
RT-PCR
-
Cell Proliferation/Viability Assay
-
Flow Cytometry
-
Cell Proliferation/Viability Assay
-
In Vivo Efficacy Study
Ver todos los productos específicos de isoformas Antibiotic
MoreVer todos los productos específicos de isoformas DNA/RNA Synthesis
More
Actividad biológica
|
Quinolone |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BT-20 | IC50 |
19 μM
Compound: Clofazimine
|
Cytotoxicity against human BT-20 cells incubated for 3 to 4 days by MTT assay
Cytotoxicity against human BT-20 cells incubated for 3 to 4 days by MTT assay
|
[PMID: 34116325] |
| HepG2 | CC50 |
49.02 μg/mL
Compound: CLFZ
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
|
[PMID: 38784457] |
| HMEC-1 | CC50 |
18.6 μM
Compound: CFM
|
Cytotoxicity against human HMEC1 cells assessed as reduction in cell viability after 72 hrs by MTT method
Cytotoxicity against human HMEC1 cells assessed as reduction in cell viability after 72 hrs by MTT method
|
[PMID: 25464882] |
| HMEC-1 | IC50 |
18.59 μM
Compound: Clofazimine
|
Cytotoxicity against HMEC1 cells after 72 hrs by MTT assay
Cytotoxicity against HMEC1 cells after 72 hrs by MTT assay
|
[PMID: 25497962] |
| Huh-7 | CC50 |
44.7 μM
Compound: 1
|
Cytotoxicity against human HuH-7 cells assessed as reduction in cell viability incubated for 24 hrs by microplate reader assay
Cytotoxicity against human HuH-7 cells assessed as reduction in cell viability incubated for 24 hrs by microplate reader assay
|
[PMID: 35279610] |
| MT4 | CC50 |
6.8 μM
Compound: CFM
|
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 96 hrs by MTT method
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 96 hrs by MTT method
|
[PMID: 25464882] |
| NIH-3T3-G185 | IC50 |
0.6 μM
Compound: Clofazimine
|
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
|
[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
1 μM
Compound: Clofazimine
|
TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
|
[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
1.1 μM
Compound: Clofazimine
|
TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
|
[PMID: 11716514] |
| Vero | IC50 |
68.6 μg/mL
Compound: CFZ
|
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
|
[PMID: 22931472] |
| Vero 76 | CC50 |
>100 μM
Compound: CFM
|
Cytotoxicity against african green monkey Vero 76 cells assessed as reduction in cell viability after 48 to 96 hrs by MTT method
Cytotoxicity against african green monkey Vero 76 cells assessed as reduction in cell viability after 48 to 96 hrs by MTT method
|
[PMID: 25464882] |
Clofazimine (0.0625-2 mg/L, 14 d) exerts no apparent activity against M. tuberculosis during the first 2–4 days of exposure, exhibits a concentration-dependent antimicrobial activity after 1 week: bacteriostatic activity at concentrations at or below the 0.25 mg/L MIC and bactericidal activity at concentrations above the MIC. INH is used as positive control.[3].
Clofazimine (10 μM, 24 h) inhibits the growth of hematological cancer cell lines (Jurkat, U266, Namalwa, K562, HL60)[4].
Clofazimine (1-50 μM, 12-48 h) shows a dose- and time-dependent inhibitory effect for U266[4].
Clofazimine (10 μM, 24-48 h) depolarizes the mitochondrial membrane, significantly increases active caspase-3 level (25-fold) and increases the percentage of early and late apoptotic cells in U266[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female BALB/c mice (age 6–8 weeks, mass 18–20 g)[3]
-
Dosage:100, 50, 25, 12.5, 6.25, 3.125 or 1.5625 mg/kg
-
Administration:Oral gavage (p.o.), once per day for 14 d
-
Result:Exhibited an increase of the lung bacterial load during the first 7 days of treatment, and decreased the CFU counts in the lungs of mice after 10 days of treatment.
Significantly declined the lung CFU counts in 100 or 50 mg/ kg group at 14th day.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 2030-63-9
-
Appearance Solid
-
Peso molecular 473.40
-
Fòrmula C27H22Cl2N4
-
Color Pink to red
-
SMILES
CC(/N=C1C(NC2=CC=C(Cl)C=C2)=CC3=NC4=C(C=CC=C4)N(C5=CC=C(Cl)C=C5)C3=C/1)C
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
Publications (13)
-
Journal Impact Factor
-
Most Recent
-
Sci Adv
A metabolic shift to the serine pathway induced by lipids fosters epigenetic reprogramming in nontransformed breast cells. [Abstract]2025 Mar 21;11(12):eads9182. PMID: 40117373
Clofazimine purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Mar 21;11(12):eads9182. [Abstract]
Clofazimine (15 μM; 24 h) significantly blocked OA-induced expression of H3K4me3-controlled genes AGR2 and PARM1, with a trend toward reduced PHGDH and NTRK2 expression in microstructures from BRCA1 wild-type individuals.
-
Commun Biol
The acetyltransferase CysE modulates virulence and drug resistance of Mycobacterium tuberculosis by interfering with oxidative stress responses. [Abstract]2025 Oct 6;8(1):1425. PMID: 41053365
Clofazimine purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 Oct 6;8(1):1425. [Abstract]
Clofazimine (CFZ) (3.125 μg/mL; 48 h) markedly reduced the survival of ΔcysE Mycobacterium tuberculosis H37Rv.
Clofazimine purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 Oct 6;8(1):1425. [Abstract]
Clofazimine (CFZ) (15.625-31.25 μg/mL; 1-3 h) strongly increased ROS levels in M. tb (Mycobacterium tuberculosis).
Clofazimine purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 Oct 6;8(1):1425. [Abstract]
Early-log-phase cultures of WT and ΔcysE M. tb (Mycobacterium tuberculosis) were treated with or without Clofazimine (CFZ) (3.125–6.25 μg/mL; 7 d). Survival was determined in the form of viable bacterial count expressed as CFU.
-
Antiviral Res
Bergamottin, a bioactive component of bergamot, inhibits SARS-CoV-2 infection in golden Syrian hamsters. [Abstract]2022 Aug:204:105365. PMID: 35732228 -
Antimicrob Agents Chemother
An enoyl-ACP reductase inhibitor, NITD-916, expresses anti- Mycobacterium abscessus activity. [Abstract]2025 May 23:e0024925. PMID: 40407337 -
Antimicrob Agents Chemother
2024 Oct 29:e0094524. PMID: 39470202 -
Antimicrob Agents Chemother
Activity of Oral Tebipenem-Avibactam in a Mouse Model of Mycobacterium abscessus Lung Infection. [Abstract]2023 Feb 16;67(2):e0145922. PMID: 36688684 -
Microbiol Spectr
In Vitro Synergy Testing of Eravacycline in Combination with Clarithromycin and Rifabutin against Mycobacterium abscessus Complex. [Abstract]2021 Sep 3;9(1):e0004521. PMID: 34132613 -
Pathogens
N-Acetylcysteine as a Host-Directed Therapy Against Clarithromycin-Resistant Mycobacterium abscessus. [Abstract]2025 Mar 21;14(4):302. PMID: 40333083 -
PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351 -
-
Clofazimine purchased from MedChemExpress. Usage Cited in: Patent. US20250312336A1.
The weights of orthotopic syngeneic pancreatic tumors from C57BL/6J mice followed treatment with ANO6 inhibitors Clofazimine (50 mg/kg; p.o.; 3 weeks).
-
-
bioRxiv
Trogocytosis of cancer-associated fibroblasts promotes pancreatic cancer growth and immune suppression via phospholipid scramblase anoctamin 6 (ANO6). [Abstract]2023 Sep 17:2023.09.15.557802. PMID: 37745612
Solvente y solubilidad
DMSO : 6.25 mg/mL (13.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
-
Ficha de datos (279 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Riccardi N, et al. Clofazimine: an old drug for never-ending diseases. Future Microbiol. 2020，15:557-566. [Content Brief]
[2]. Arbiser JL, et al. Clofazimine: a review of its medical uses and mechanisms of action. J Am Acad Dermatol. 1995 Feb;32(2 Pt 1):241-7. [Content Brief]
[3]. Ammerman NC, et al. Clofazimine has delayed antimicrobial activity against Mycobacterium tuberculosis both in vitro and in vivo. J Antimicrob Chemother. 2017，72(2):455-461. [Content Brief]
[4]. Durusu İZ, et al. Anti-cancer effect of clofazimine as a single agent and in combination with cisplatin on U266 multiple myeloma cell line. Leuk Res. 2017，55:33-40. [Content Brief]
[5]. Ren YR, et al. Clofazimine Inhibits Human Kv1.3 Potassium Channel by Perturbing Calcium Oscillation in T Lymphocytes. PLoS One. 2008，3(12):e4009. [Content Brief]
[6]. Cholo MC, et al. Clofazimine: current status and future prospects. J Antimicrob Chemother. 2012 Feb;67(2):290-8. [Content Brief]
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1124 mL | 10.5619 mL | 21.1238 mL | 52.8095 mL |
| 5 mM | 0.4225 mL | 2.1124 mL | 4.2248 mL | 10.5619 mL | |
| 10 mM | 0.2112 mL | 1.0562 mL | 2.1124 mL | 5.2809 mL |
Clofazimine Related Classifications
HY-B1046 Related Classifications
Powered by Bioz