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PSMA targeting peptide TFA (PSMA-1 TFA) is a PSMA targeting peptide (GRFLTGGTGRLLRIS) and can be used for targeted delivery of glucose-regulated protein (GRP)-silencing siRNAs in PCa cells .
pNPS-DHA (Compound 19) is an orally active DHA-ethanolamide (DHEA) derivative that has antiallergic activity. pNPS-DHA inhibits IgE-dependent passive cutaneous anaphylaxis (PCA) reaction in mice. pNPS-DHA has anti-degranulating activity in RBL-2H3 mast cells with an IC50 of 15 μM .
PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor. VPC-13566 is effective in inhibiting AR transcriptional activity in vitro as well as the growth of AR-dependent PCa cell lines. VPC-13566 can be used as a chemical probe to help identify unknown AR partners.VPC-13566 can be used for the research of cancer.
SLU-PP-1072 is a dual ERRα/γ inverse agonist, used in Prostate cancer (PCa) research. SLU-PP-1072 disrupts PCa cell metabolism, and induces apoptosis via dysregulating cell cycle .
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .
Isosilybin A (Standard) is the analytical standard of Isosilybin A. This product is intended for research and analytical applications. Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .
Tixanox sodium (RS-7540), an anti-allergic compound, is a potent inhibitor of mediator release in the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction .
Cloxacepride is an orally active and potent antiallergic agent. Cloxacepride is a CaM (calmodulin) antagonist. Cloxacepride has anti-PCA (passive cutaneous anaphylaxis) activity .
PSMA-1 is a PSMA targeting peptide (GRFLTGGTGRLLRIS) and can be used for for targeted delivery of glucose-regulated protein (GRP)-silencing siRNAs in PCa cells. PSMA-1 is selected and polyarginine sequences R6 or R9 were added at the C terminus to generate the CTPs. FITC labeling of the peptide with an aminohexanoic acid (Ahx) linker at the N terminus produced FITC-PSMA-1, to track PSMA binding on PCa cells .
PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
PSMA I&T is an effective inhibitor of prostate-specific membrane antigen (PSMA). PSMA I&T can be used for SPECT/CT imaging and radionuclide studies in triple-negative breast cancer and prostate cancer (PCa) .
Elbanizine inhibits histamine, bradykinin, histamin-release from rat mast cells (IC50 of 0.26 μM) and the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction. Elbanizine exhibits antiallergic and antiasthmatic in guinea pig model .
Gymnoside I (compound 1) is a glycosidoxybenzyl 2-isobutylmalic acid. Gymnoside I shows antiallergic activity in passive cutaneous allergic reaction (PCA) in mice. Gymnoside I can be used in research to treat asthma, neurasthenia and chronic hepatitis .
Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation .
Senaparib hydrochloride (IMP4297 hydrochloride) is an oral, selective PARP1/2 inhibitor with potent anti-tumor activity. Senaparib hydrochloride shows antitumor activity against advanced ovarian cancer .
Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models .
2-Heptyl-4-quinolone is an intermediate in the synthesis of the Pseudomonas quinolone signal (PQS) that controls swarming by positively regulating phenazine production. 2-Heptyl-4-quinolone induces the production of the phenazine-1-carboxylic acid (PCA) .
GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells .
Spinacetin is a natural product that can be isolated from Inula japonica. Spinacetin inhibits the release of histamine. Spinacetin has anti-inflammatory activity .
Isosilybin B (Standard) is the analytical standard of Isosilybin B. This product is intended for research and analytical applications. Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation .
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a human monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKT activation .
Methyl p-coumarate (Methyl 4-hydroxycinnamate), an orally active esterified derivative of p-Coumaric acid (pCA), can be isolated from the flower of Trixis michuacana var longifolia. Methyl p-coumarate could inhibit the melanin formation in B16 mouse melanoma cells. Methyl p-coumarate also has strong in vitro inhibitory effect on A. alternata and other pathogens .
3-Hydroxybenzaldehyde (3-HBA) is a precursor compound for phenolic compounds like Protocatechuic aldehyde (PCA) (HY-N0295). 3-Hydroxybenzaldehyde, produced by 3-hydroxybenzyl-alcohol dehydrogenase, is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans. 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo. 3-Hydroxybenzaldehyde is proming for research of atherosclerosis .
OB-24 is a potent inhibitor of heme oxygenase-1 (HO-1). Heme oxygenase-1, a member of the heat shock protein family, plays a key role as a sensor and regulator of oxidative stress. OB-24 significantly inhibited cell proliferation in vitro and tumor growth and lymph node/lung metastases in vivo. OB-24 has potential for the research of advanced prostate cancer (PCA) .
YT 6-2 is the p62/SQSTM1 targeting, autophagy-targeting ligand (ATL) of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa .
HDAC-IN-64 (Compound 13) is a HDAC inhibitor. HDAC-IN-64 inhibits HDAC4/5/6/7/9 with IC50s of 24, 45, 85, 31, 37 nM. HDAC-IN-64 has anti-proliferative activity and anti-migration properties on prostate cancer (PCA) cells. HDAC-IN-64 inhibits LNCaP and RWPE-1 cell growth with GI50 of 0.32 and 1.1 μM respectively .
2-Heptyl-4-quinolone- 13C6 is the 13C-labeled 2-Heptyl-4-quinolone (HY-129503). 2-Heptyl-4-quinolone is an intermediate in the synthesis of the Pseudomonas quinolone signal (PQS) that controls swarming by positively regulating phenazine production. 2-Heptyl-4-quinolone induces the production of the phenazine-1-carboxylic acid (PCA) .
2-Heptyl-4-quinolone- 15N is the 15N-labeled 2-Heptyl-4-quinolone (HY-129503). 2-Heptyl-4-quinolone is an intermediate in the synthesis of the Pseudomonas quinolone signal (PQS) that controls swarming by positively regulating phenazine production. 2-Heptyl-4-quinolone induces the production of the phenazine-1-carboxylic acid (PCA) .
DR-4004 is a 5-HT7 receptor antagonist that attenuates the decreased level of performance produced by mCPP and the performance levels after p-chloroamphetamine (PCA) lesion of the 5-HT system. DR-4004 also reverses amnesia induced by Scopolamine (HY-N0296) and Dizocilpine (HY-15084B). DR-4004 is promising for research of schizophrenia, cognitive deficits and atypical antipsychotic agents .
BKIDC-1553 is an orally active antiglycolytic agent and a bumped kinase inhibitor derived compound with a predicted ~17 h half-life in human. BKIDC-1553 inhibits CYP2C8 and Angiotensin Converting Enzyme and can be used for cancer research .
YT 6-2 analog-1 (compound 2-3) is the p62/SQSTM1 targeting, autophagy-targeting ligand (ATL) of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa .
YT 6-2-PEG3-C2-NH2 is the p62/SQSTM1 targeting, autophagy-targeting ligand-linker conjugate of AUTOTAC ATC-324 (HY-169385), which is an bivalent AR (Androgen Receptor) degrader. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa .
MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29?μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52?μM and unstresses RPMI 8226 cells with an IC50 of 0.14?μM . MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth .
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .
Procyanidin B2, 3,3'-di-O-gallate is an active constituent. Procyanidin B2, 3,3'-di-O-gallate can be isolated from grape seed extract (GSE) procyanidin mix. Procyanidin B2, 3,3' -di-o-gallate target cancer stem cells (CSCs) in prostate cancer (PCa). Procyanidin B2, 3,3'-di-O-gallate targets both unsorted and sorted CSCs at lower doses. Procyanidin B2, 3,3'-di-O-gallate strongly suppresses the constitutive as well as Jagged1 (Notch1 ligand)-induced activated Notch1 pathway .
Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K + channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research .
ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa . ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).
Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription . Lycorine is also a melanoma vasculogenic inhibitor . Lycorine can be used for the study of prostate cancer and metabolic diseases .
Cancer is one of the leading causes of mortality amongst world’s population, in which prostate cancer (PCa) is one of the most encountered malignancies among men. Several molecular mechanisms are involved in prostate cancer development and progression. These include common survival factors in prostate cancer (IGF-1), growth factors (TGF-α, EGF), Wnt, Hedgehog, NF-κB, and mTOR and other signaling pathways. These provide potential therapeutic target in prostate cancer treatment.
MCE offers a unique collection of 2,666 compounds with identified and potential anti-prostate cancer activity. MCE Anti-Prostate Cancer Compound Library is a useful tool for anti-prostate cancer drugs screening and other related research.
PSMA targeting peptide TFA (PSMA-1 TFA) is a PSMA targeting peptide (GRFLTGGTGRLLRIS) and can be used for targeted delivery of glucose-regulated protein (GRP)-silencing siRNAs in PCa cells .
PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
PSMA-1 is a PSMA targeting peptide (GRFLTGGTGRLLRIS) and can be used for for targeted delivery of glucose-regulated protein (GRP)-silencing siRNAs in PCa cells. PSMA-1 is selected and polyarginine sequences R6 or R9 were added at the C terminus to generate the CTPs. FITC labeling of the peptide with an aminohexanoic acid (Ahx) linker at the N terminus produced FITC-PSMA-1, to track PSMA binding on PCa cells .
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a human monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKT activation .
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .
Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation .
Spinacetin is a natural product that can be isolated from Inula japonica. Spinacetin inhibits the release of histamine. Spinacetin has anti-inflammatory activity .
Methyl p-coumarate (Methyl 4-hydroxycinnamate), an orally active esterified derivative of p-Coumaric acid (pCA), can be isolated from the flower of Trixis michuacana var longifolia. Methyl p-coumarate could inhibit the melanin formation in B16 mouse melanoma cells. Methyl p-coumarate also has strong in vitro inhibitory effect on A. alternata and other pathogens .
3-Hydroxybenzaldehyde (3-HBA) is a precursor compound for phenolic compounds like Protocatechuic aldehyde (PCA) (HY-N0295). 3-Hydroxybenzaldehyde, produced by 3-hydroxybenzyl-alcohol dehydrogenase, is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans. 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo. 3-Hydroxybenzaldehyde is proming for research of atherosclerosis .
Isosilybin A (Standard) is the analytical standard of Isosilybin A. This product is intended for research and analytical applications. Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .
Gymnoside I (compound 1) is a glycosidoxybenzyl 2-isobutylmalic acid. Gymnoside I shows antiallergic activity in passive cutaneous allergic reaction (PCA) in mice. Gymnoside I can be used in research to treat asthma, neurasthenia and chronic hepatitis .
2-Heptyl-4-quinolone is an intermediate in the synthesis of the Pseudomonas quinolone signal (PQS) that controls swarming by positively regulating phenazine production. 2-Heptyl-4-quinolone induces the production of the phenazine-1-carboxylic acid (PCA) .
Isosilybin B (Standard) is the analytical standard of Isosilybin B. This product is intended for research and analytical applications. Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation .
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .
Procyanidin B2, 3,3'-di-O-gallate is an active constituent. Procyanidin B2, 3,3'-di-O-gallate can be isolated from grape seed extract (GSE) procyanidin mix. Procyanidin B2, 3,3' -di-o-gallate target cancer stem cells (CSCs) in prostate cancer (PCa). Procyanidin B2, 3,3'-di-O-gallate targets both unsorted and sorted CSCs at lower doses. Procyanidin B2, 3,3'-di-O-gallate strongly suppresses the constitutive as well as Jagged1 (Notch1 ligand)-induced activated Notch1 pathway .
Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription . Lycorine is also a melanoma vasculogenic inhibitor . Lycorine can be used for the study of prostate cancer and metabolic diseases .
ENPP-1 protein is a nucleotide pyrophosphatase that inhibits excessive hydroxyapatite crystal growth by preferentially hydrolyzing ATP and other nucleoside triphosphates to generate PPi, thereby critically regulating bone mineralization and soft tissue calcification. ENPP-1 Protein, Human (HEK293, His) is the recombinant human-derived ENPP-1 protein, expressed by HEK293 , with C-His labeled tag. The total length of ENPP-1 Protein, Human (HEK293, His) is 828 a.a., with molecular weight of 110-120 kDa.
ENPP-1 is a nucleotide pyrophosphatase that critically regulates bone mineralization and soft tissue calcification through the production of diphosphate (PPi).This PPi inhibits the growth of hydroxyapatite crystals and prevents unwanted mineralization.ENPP-1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived ENPP-1 protein, expressed by HEK293 , with C-His labeled tag.
ENPP-1 protein is a nucleotide pyrophosphatase that inhibits excessive hydroxyapatite crystal growth by preferentially hydrolyzing ATP and other nucleoside triphosphates to generate PPi, thereby critically regulating bone mineralization and soft tissue calcification. ENPP-1 Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived ENPP-1 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of ENPP-1 Protein, Human (Biotinylated, HEK293, His-Avi) is 828 a.a., with molecular weight of 110-120 kDa.
2-Heptyl-4-quinolone- 13C6 is the 13C-labeled 2-Heptyl-4-quinolone (HY-129503). 2-Heptyl-4-quinolone is an intermediate in the synthesis of the Pseudomonas quinolone signal (PQS) that controls swarming by positively regulating phenazine production. 2-Heptyl-4-quinolone induces the production of the phenazine-1-carboxylic acid (PCA) .
2-Heptyl-4-quinolone- 15N is the 15N-labeled 2-Heptyl-4-quinolone (HY-129503). 2-Heptyl-4-quinolone is an intermediate in the synthesis of the Pseudomonas quinolone signal (PQS) that controls swarming by positively regulating phenazine production. 2-Heptyl-4-quinolone induces the production of the phenazine-1-carboxylic acid (PCA) .
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