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PFI

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Autophagy (1) Biochemical Assay Reagents (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (6) Histone Demethylase (1) Histone Methyltransferase (5) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (1) Pantetheinase (1) SWI/SNF Complex (1)
By Research Areas:	Cancer (13) Infection (2) Inflammation/Immunology (3) Metabolic Disease (1)

Inhibitors & Agonists

Fluorescent Dye

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18627A

PFI-2 hydrochloride Maximum Cited Publications 14 Publications Verification (R)-PFI-2 hydrochloride	Histone Methyltransferase	Infection Inflammation/Immunology Cancer
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC₅₀ value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC₅₀ value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis .

HY-12409

PFI-3 5 Publications Verification	Epigenetic Reader Domain	Cancer
PFI-3, a chemical probe, is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a K_d of 89 nM.

HY-18627

PFI-2 Maximum Cited Publications 14 Publications Verification (R)-PFI-2	Histone Methyltransferase	Infection Inflammation/Immunology Cancer
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride, a chemical probe, is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC₅₀ value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC₅₀ value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis .

HY-139348

PFI-90 1 Publications Verification	Histone Demethylase Apoptosis	Cancer
PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. PFI-90 induces apoptosis and myogenic differentiation, resulting in the cell death increased. PFI-90 has the potential for the antitumor activity. (patent WO2021101929A1).

HY-16586

PFI-1 3 Publications Verification	Epigenetic Reader Domain Autophagy Apoptosis	Cancer
PFI-1, a chemical probe, is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC₅₀ of 0.22 μM in a cell-free assay.

HY-18664

PFI-4 3 Publications Verification	Epigenetic Reader Domain	Cancer
PFI-4 (compound 11), a chemical probe, is a potent and highly selective BRPF1 Bromodomain (BRPF1B) inhibitor, with an IC₅₀ of 172 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions .

HY-129035

PFI-653 Vanin-1-IN-1	Pantetheinase	Metabolic Disease Inflammation/Immunology
PFI-653 (Vanin-1-IN-1, compound 3), a chemical probe, is a vanin-1 inhibitor that binds to plasma vanin-1 from mouse, rat, dog, and human. Vanin-1 is a cell surface-associated inositol (GPi) -anchored protein that plays important roles in metabolism and inflammation. PFI-653 inhibits vanin-1 from different species with IC₅₀s of 6.85 nM (human recombinant plasma vanin-1), 9.0 nM (human plasma vanin-1), 24.5 nM (mouse recombinant vanin-1), and 53.4 nM (mouse plasma vanin-1) .

HY-155412

PFI-6	Epigenetic Reader Domain	Cancer
PFI-6 is a selective MLLT1 and MLLT3 YEATS domain probe with IC₅₀ values of 0.14 μM and 0.16 μM, respectively. PFI-6 is applicable for cancer research .

HY-152242

YEATS4-IN-1 PFI-8	Histone Methyltransferase	Others
YEATS4-IN-1 (Compound 4d) is a potent and selective YEATS4 binder that binds to the KAc recognition site of the YEATS structural domain with a K_i value of 33 nM .

HY-144720

BRG1-IN-1	SWI/SNF Complex	Cancer
BRG1-IN-1 (Compound 11d) is a potent inhibitor of SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors .

HY-D2259

PFI-7	E1/E2/E3 Enzyme Ligands for E3 Ligase	Others
PFI-7 is a probe, which binds to human GID4 (K_D is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .

HY-169094

PFI-6-COOH	Epigenetic Reader Domain Ligands for Target Protein for PROTAC	Cancer
PFI-6-COOH (Compound 18) is an eleven-nineteen leukemia (ENL) ligand, and can be used for synthesis of MS41 (HY-169093), an ENL PROTAC degrader .

HY-176821

PFI-6N	Biochemical Assay Reagents	Cancer
PFI-6N is a negative control compound of PFI-6 (HY-155412). PFI-6N is completely inactive against YEATS domain (MLLT1/3 and YEATS2/4) by methylating the amide of PFI-6 .

HY-110196

*(S)-PFI-2 hydrochloride*	Histone Methyltransferase	Others
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .

HY-174997

PFI-7-O-C4-piperazin	E3 Ligase Ligand-Linker Conjugates	Cancer
PFI-7-O-C4-piperazin is a E3 ligase ligand-linker conjugate that can be used for synthesis of PROTACs, such as NEP162 (HY-174996). The E3 ligase ligand (PFI-7) of NEP162 is a highly selective antagonist of GID4 (K_D = 0.22 μM). NEP162 is a BRD4 PROTAC degrader with anti-tumor activity ^{[1] ^.}

HY-156455

SETD7-IN-1	Histone Methyltransferase	Cancer
SETD7-IN-1 (compound 7) is a PFI-2 (HY-18627) analogue. SETD7-IN-1 is a substrate and inhibitor of histone lysine methyltransferase SETD7, with an IC₅₀ of 0.96 ± 0.10 µM .

HY-122573

Bromodomain inhibitor-13	Epigenetic Reader Domain	Cancer
Bromodomain inhibitor-13 (Compound 1) is an analog of PFI-3 (HY-12409). Bromodomain inhibitor-13 is a bromodomain-containing protein (BCP) inhibitor. Bromodomain inhibitor-13 targets SMARCA2, SMARCA4, PB1(5), and second bromodomain of PB1 (PB1(2)) with K_D values of 37, 53, 30, and 190 nM, respectively .

PFI-7	Fluorescent Dye
PFI-7 is a probe, which binds to human GID4 (K_D is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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