1. Metabolic Enzyme/Protease Anti-infection Apoptosis
  2. Phosphoglycerate Kinase (PGK) Fungal Apoptosis
  3. Ilicicolin H

Ilicicolin H is a selective and non-ATP-competitive phosphoglycerate kinase 1 (PGK1) (IC50 = 9.02 μM) and mitochondrial cytochrome bc1 reductase (IC50 = 2-3 ng/mL) inhibitor. Ilicicolin H directly binds to PGK1 with KD of 60 μM .Ilicicolin H can inhibit cell proliferation and induce apoptosis. Ilicicolin H can inhibit the lactate production and glucose uptake of hepatocellular carcinoma (HCC) cells. Ilicicolin H has a broad antifungal spectrum including C. albicans, Cryptococcus and A. fumigatus. Ilicicolin H can be used for the researches of cancer and infection, such as hepatocellular carcinoma (HCC) and C. albicans infection.

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

Ilicicolin H

Ilicicolin H Chemical Structure

CAS No. : 12689-26-8

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500 μg In-stock

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Description

Ilicicolin H is a selective and non-ATP-competitive phosphoglycerate kinase 1 (PGK1) (IC50 = 9.02 μM) and mitochondrial cytochrome bc1 reductase (IC50 = 2-3 ng/mL) inhibitor. Ilicicolin H directly binds to PGK1 with KD of 60 μM .Ilicicolin H can inhibit cell proliferation and induce apoptosis. Ilicicolin H can inhibit the lactate production and glucose uptake of hepatocellular carcinoma (HCC) cells. Ilicicolin H has a broad antifungal spectrum including C. albicans, Cryptococcus and A. fumigatus. Ilicicolin H can be used for the researches of cancer and infection, such as hepatocellular carcinoma (HCC) and C. albicans infection[1][2].

IC50 & Target[1]

PGK1

9.02 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
4T1 IC50
13.84 μM
Compound: 10
Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
A549 IC50
7.01 μM
Compound: 10
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
B16-F10 IC50
21.58 μM
Compound: 10
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
CT26 IC50
19.54 μM
Compound: 10
Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
HCT-116 IC50
10.75 μM
Compound: 10
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
MC-38 IC50
19.55 μM
Compound: 10
Cytotoxicity against mouse MC38 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse MC38 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
MDA-MB-231 IC50
9.98 μM
Compound: 10
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
MDA-MB-435 IC50
6.34 μM
Compound: 10
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
NCI-H1703 IC50
6.65 μM
Compound: 10
Cytotoxicity against human NCI-H1703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human NCI-H1703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
PC-3 IC50
> 50 μM
Compound: 10
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
SNB-19 IC50
14.59 μM
Compound: 10
Cytotoxicity against human SNB-19 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human SNB-19 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 38527379]
In Vitro

Ilicicolin H (1-8 μM, 24 h) induces apoptosis and increases active cleaved fragments of Caspase-3, Caspase-9 levels in HepG2 and Huh7 cells[1].
Ilicicolin H (2-8 μM, 6 h) reduces the levels of HIF-1α induced by CoCl 2 and the phosphorylation levels of PDHK1 at T338 induced by EGF in HepG2 cells[1].
Ilicicolin H (1-8 μM, 6 h) inhibits lactate production and glucose uptake in HepG2 cells[1].
Ilicicolin H shows anti-fungal activity against C. albicans (0.04 to 0.31 μg/mL), other Candida species (0.01 to 5.0 μg/mL), Cryptococcus (MIC = 0.1-1.56 μg/mL) and A. fumigatus (MIC = 0.08 μg/mL)[2].

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

Apoptosis Analysis[1]

Cell Line: HepG2 and Huh7 cells
Concentration: 1, 2, 4 and 8 μM
Incubation Time: 24 h
Result: Increased C-Cas3, C-Cas9, and C-Parp levels.
Increased apoptotic cells.
In Vivo

Ilicicolin H (6.25-50 mg/kg, p.o., daily for 2 days) reduces C. albicans burden in C. albicans infected mice models[2].

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

Animal Model: C. albicans infected mice models[2]
Dosage: 6.25, 12.5, 25 and 50 mg/kg
Administration: Orally administration, daily for 2 days
Result: Reduced C. albicans burden.
Molecular Weight

433.54

Formula

C27H31NO4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(C([C@H]2[C@H](/C=C/C)[C@@]3([H])C[C@@H](C)CC[C@]3([H])C(C)=C2)=O)=C(O)C(C4=CC=C(O)C=C4)=CN1

Structure Classification
Initial Source

Campylocarpon sp.

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ilicicolin H
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