F2F-202
F2F-202 is a selective HDAC6 inhibitor with an IC50 of 7.1 nM, exhibiting high selectivity toward HDAC1. F2F-202 does not directly bind to or inhibit the Hda1 protease activity of Candida albicans itself, but reduces the mRNA transcription level of the Hda1 gene. When combined with Voriconazole (HY-76200), F2F-202 decreases the yeast-hypha transition rate of azole-resistant Candida albicans and impairs the antioxidant response of azole-resistant Candida albicans. F2F-202 can be used in studies related to azole-resistant Candida albicans infections.
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- 화학식: C36H45N5O6
- 분자량:643.77
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
HDAC6 7.1 nM (IC50) |
HDAC1 2192 nM (IC50) |
In Vitro
F2F-202 (25-400 μM; 24 h) alone does not significantly inhibit the growth of azole-sensitive Candida albicans ATCC 90028, but when applied at concentrations of 100-400 μM for 24 h, it causes a moderate concentration-dependent reduction (12-26%) in the growth of azole-resistant Candida albicans ATCC 10231[1].
F2F-202 (100 μM; 1-6 days) exerts a synergistic effect with Voriconazole (FICI = 0.129), completely inhibiting the long-term (6-day) growth of azole-resistant C. albicans ATCC 10231 and abrogating the trailing effect of azole-susceptible C. albicans ATCC 90028[1].
F2F-202 (100 μM; 2-24 h) alone does not inhibit yeast-hypha transition of Candida albicans ATCC 10231, but when combined with Voriconazole, it significantly reduces hypha formation and promotes the maintenance of yeast morphology after 24 h of treatment at 37 °C[1].
F2F-202 (100 μM; 2-24 h) regulates the expression of genes associated with virulence, stress response and azole resistance in Candida albicans ATCC 10231; its efficacy is enhanced when used in combination with Voriconazole, including significant down-regulation of Als1 and Hwp1 expression, as well as inhibition of Voriconazole-induced up-regulation of Erg11[1].
F2F-202 (100 μM; 24 h) alone does not induce intracellular ROS production in Candida albicans ATCC 10231, but when combined with Voriconazole, it significantly enhances Voriconazole-induced oxidative stress after 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:azole-resistant Candida albicans ATCC 10231
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Concentration:100 μM; 100 μM (in combination with 0.125 μg/mL Voriconazole)
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Incubation Time:2 h, 24 h
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Result:Reduced Hda1 expression by 50%, reduced Als1 expression by 41%, and increased Sod1 expression by 55% after 2 h when used alone; had no significant effect on Nrg1, Hwp1, or Erg11 expression.
Reduced Nrg1 expression by 52%, had a marginal nonsignificant reduction in Als1 expression (18%), and had no significant effect on Hda1, Hwp1, Erg11, or Sod1 expression after 24 h when used alone.
In combination with voriconazole after 2 h: reduced Hda1 expression by 64%, reduced Als1 expression by 87%, reduced Sod1 expression by 48%, and partially attenuated voriconazole-induced Erg11 upregulation (resulting in a nonsignificant 36% increase vs. control).
In combination with voriconazole after 24 h: reduced Hwp1 expression by 79%, reduced Als1 expression by 51%, and strongly attenuated voriconazole-induced Erg11 upregulation (resulting in a nonsignificant increase vs. control).
Chemical Information
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분자량 643.77
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화학식 C36H45N5O6
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SMILES
O=C(OC(C)(C)C)N[C@H]([C@H](O)CN(CC1)CCC1(N(C2=CC=CC=C2)CN3CC4=CC=C(C(NO)=O)C=C4)C3=O)CC5=CC=CC=C5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1].
Barone S, et al. F2F-202, a Selective Histone Deacetylase 6 (HDAC6) Inhibitor, Behaves as an Arrow with Multiple Tips against Azole-Resistant C. albicans: Modulation of Yeast-to-Hyphae Transition, Trailing Effect, and Oxidative Stress. ACS Infect Dis. 2026 Jun 12;12(6):2101-2113.
[Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
F2F-202 Related Classifications
HY-184165 Related Classifications
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