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LnCAP

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237

Inhibitors & Agonists

3

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1

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6

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3

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34

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7

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3

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-70002
    Enzalutamide
    Maximum Cited Publications
    214 Publications Verification

    MDV3100

    		 Androgen Receptor Autophagy Cancer
    Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .
    Enzalutamide
  • HY-N0528
    Linarin
    4 Publications Verification

    Buddleoside; Linarine

    		 TNF Receptor Cholinesterase (ChE) PKA Apoptosis Bacterial HIV Influenza Virus Infection Neurological Disease Inflammation/Immunology Cancer
    Linarin (Buddleoside) is an orally active and selective inhibitor of acetylcholinesterase (AChE). Linarin has many activities, such as anti-inflammatory, antioxidant, sleep aid and sedation, bone differentiation, anti-tumor, antibacterial and antiviral. Linarin can be used to study diseases such as the nervous system, osteoporosis and cancer .
    Linarin
  • HY-158113
    CBPD-409

    		Histone Acetyltransferase PROTACs Cancer
    CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
    CBPD-409
  • HY-N2908
    Atraric acid

    Methyl atrarate

    		 Environmental Pollutants NF-κB Androgen Receptor p38 MAPK NO Synthase Inflammation/Immunology Cancer
    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 .
    Atraric acid
  • HY-113332
    Myristoleic acid
    1 Publications Verification

    		 Environmental Pollutants Endogenous Metabolite Apoptosis Inflammation/Immunology
    Myristoleic acid, a cytotoxic component in the extract from Serenoa repens, induces apoptosis and necrosis in human prostatic LNCaP cells .
    Myristoleic acid
  • HY-70002R
    Enzalutamide (Standard)

    MDV3100 (Standard)

    		 Reference Standards Androgen Receptor Autophagy Cancer
    Enzalutamide (Standard) is the analytical standard of Enzalutamide. This product is intended for research and analytical applications. Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .
    Enzalutamide (Standard)
  • HY-13941
    1-Naphthyl PP1
    3 Publications Verification

    1-NA-PP 1

    		 Src PKD Neurological Disease Inflammation/Immunology Cancer
    1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases and Protein Kinase D. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively .
    1-Naphthyl PP1
  • HY-70002S1
    Enzalutamide-d6

    MDV3100-d6

    		 Isotope-Labeled Compounds Androgen Receptor Cancer
    Enzalutamide-d6 (MDV3100-d6) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
    Enzalutamide-d6
  • HY-16079
    AZD3514
    3 Publications Verification

    		 Androgen Receptor Cancer
    AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer .
    AZD3514
  • HY-111875
    SNIPER(BRD)-1

    		SNIPERs PROTACs Epigenetic Reader Domain Cancer
    SNIPER(BRD)-1 is a SNIPER degrader of BRD4, cIAP1 and XIAP. SNIPER(BRD)-1 has IC50 values of 6.8 nM, 17 nM and 49 nM for cIAP1, cIAP2 and XIAP, respectively. SNIPER(BRD)-1 can be used for cancer research . (Blue: LCL161 (HY-15518); Black: linker (HY-W008005); Pink: (+)-JQ-1 (HY-13030))
    SNIPER(BRD)-1
  • HY-130992
    Androgen receptor antagonist 1

    		Androgen Receptor Ligands for Target Protein for PROTAC Cancer
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM . Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively .
    Androgen receptor antagonist 1
  • HY-70002S
    Deutenzalutamide

    Enzalutamide-d3; MDV3100-d3

    		 Androgen Receptor Autophagy Cancer
    Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
    Deutenzalutamide
  • HY-115282A
    JNJ-63576253
    1 Publications Verification

    TRC-253

    		 Androgen Receptor Cancer
    JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
    JNJ-63576253
  • HY-149433
    BWA-522

    		PROTACs Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .
    BWA-522
  • HY-13626
    Spisulosine
    1 Publications Verification

    ES-285

    		 PKC Apoptosis Cancer
    Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation. Spisulosine induces apoptosis in PC-3 and LNCaP cells .
    Spisulosine
  • HY-170329
    PROTAC AR Degrader-8

    		PROTACs Androgen Receptor Apoptosis Cancer
    PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC50s of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 values of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer .
    PROTAC AR Degrader-8
  • HY-P10816
    PACE4 Inhibitory peptide C23

    Ac-(DLeu)LLLRVK-Amba

    		 Bacterial Infection Cancer
    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 .
    PACE4 Inhibitory peptide C23
  • HY-147291
    VPC-70063

    		c-Myc PARP Apoptosis Cancer
    VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 reduces UBE2C promotor activity and AR-V7 levels, and induces PARP cleavage. VPC-70063 induces apoptosis and blocks Myc-Max interactions with DNA. VPC-70063 can be used for researching anticancer .
    VPC-70063
  • HY-151538
    PBRM1-BD2-IN-8

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity .
    PBRM1-BD2-IN-8
  • HY-133045
    VHL Ligand 8

    		Ligands for E3 Ligase Cancer
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
    VHL Ligand 8
  • HY-N12124
    Monascuspiloin

    Monascinol

    		 Akt mTOR AMPK Androgen Receptor Apoptosis Autophagy Cancer
    Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice .
    Monascuspiloin
  • HY-149862
    ARD-2051
    1 Publications Verification

    		 PROTACs Androgen Receptor Cancer
    ARD-2051 is a selective and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .
    ARD-2051
  • HY-144667
    ALDH1A3-IN-1

    		Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH1A3-IN-1 (Compound 14) is a potent ALDH1A3 inhibitor, with an IC50 of 0.63 μM and a Ki of 0.46 μM. ALDH1A3-IN-1 can be studied in prostate cancer .
    ALDH1A3-IN-1
  • HY-N7510
    12-O-Methylcarnosic acid

    12-Methoxycarnosic acid

    		 5 alpha Reductase Infection Cancer
    12-O-Methylcarnosic acid (12-Methoxycarnosic acid), a diterpene carnosic acid isolated from the acetone extract of Salvia microphylla, is an active constituent of 5α-reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid inhibits proliferation in LNCaP cells. 12-O-Methylcarnosic acid has antioxidant, anti-cancer and antimicrobial activity .
    12-O-Methylcarnosic acid
  • HY-141487
    CLP-3094
    2 Publications Verification

    		 Androgen Receptor Metabolic Disease Inflammation/Immunology
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM) . CLP-3094 is a selective, potent GPR142 antagonist .
    CLP-3094
  • HY-151532
    PBRM1-BD2-IN-5

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer .
    PBRM1-BD2-IN-5
  • HY-N3999
    Venuloside A

    ESK246

    		 Others Cancer
    Venuloside A is a potent inhibitor of LAT3. Venuloside A inhibits the leucine uptake in LNCaP prostate cancer cells with an IC50 of 8.12 μM .
    Venuloside A
  • HY-163572
    PIP5K1α-IN-1

    		PI4P5K Cancer
    PIP5K1α-IN-1 (Compound 3e) is an inhibitor for phosphatidylinositol 4-phosphate 5-kinase type I α (PIP5K1α) with an IC50 of 0.46 μM .
    PIP5K1α-IN-1
  • HY-163641
    AR Degrader-1

    		Molecular Glues Androgen Receptor E1/E2/E3 Enzyme Cancer
    AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells .
    AR Degrader-1
  • HY-150268
    Zavabresib

    BET-IN-16

    		 Epigenetic Reader Domain Cancer
    Zavabresib (BET-IN-16) (Compound I) is a BET inhibitor. BET-IN-16 shows anticancer activity. Zavabresib inhibits prostate cancer cell growth, with IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively .
    Zavabresib
  • HY-N16483
    Procyanidin B2-3'-O-gallate

    		Apoptosis Caspase Bcl-2 Family PARP Androgen Receptor Cancer
    Procyanidin B2-3'-O-gallate is a mono-gallate ester that can be isolated from grape seed extract. Procyanidin B2-3'-O-gallate has anti-cancer efficacy and reduces the viability of prostate carcinoma LNCaP cells. Furthermore, Procyanidin B2-3'-O-gallate induces apoptosis, and causes caspases-9 and -3 and PARP cleavage, and down-regulates Bcl-2, Bcl-Xl and androgen receptor levels .
    Procyanidin B2-3'-O-gallate
  • HY-175455
    LYA914

    		PROTACs Androgen Receptor Akt Cancer
    LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .
    LYA914
  • HY-176128
    BWA-6047

    		PROTACs Androgen Receptor Apoptosis PARP Caspase Cancer
    BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
    BWA-6047
  • HY-W748509
    Pipernonaline

    		Caspase Apoptosis Cancer
    Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
    Pipernonaline
  • HY-121088
    Ceefourin 2

    		P-glycoprotein Cardiovascular Disease Others
    Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability .
    Ceefourin 2
  • HY-Y0943
    Isobutyramide

    		Drug Metabolite Cancer
    Aldehyde Dehydrogenase Isobutyramide is an orally active liver alcohol dehydrogenase (LADH2) inhibitor. Isobutyramide inhibits ethanol metabolism and enhances differentiation-related gene expression, inducing cell cycle arrest and significantly reducing the growth rate of prostate cancer cells (LNCaP). Isobutyramide is promising for research of advanced prostate cancer .
    Isobutyramide
  • HY-105314
    LY-33169

    		Others Cancer
    LY-33169 is an antitumor agent. LY-33169 had selective cytotoxicity against Colon Adenocarcinoma-38, Human Colon-116, Human Prostate LNCaP, and Human Breast WSU-Br-1 cells .
    LY-33169
  • HY-N16066
    Candidusin A

    CHNQD-0803

    		 AMPK Apoptosis NF-κB TNF Receptor Inflammation/Immunology
    Candidusin A (CHNQD-0803) (Compound 4) is a AMPK activator with a KD of 47.28 nM. Candidusin A can be isolated from marine fungus Aspergillus candidus. Candidusin A has cytotoxic activity and induces apoptosis in human prostate cancer cells (22Rv1, PC-3 and LNCaP cells). Candidusin A reduces adipogenesis genes expression and fat deposition, negatively regulates the NF-κB-TNFα inflammatory axis to suppress inflammation, and ameliorates liver injury and fibrosis. Candidusin A can be used for non-alcoholic steatohepatitis (NASH) research .
    Candidusin A
  • HY-168757
    PSMA precursor-1

    		PSMA Cancer
    PSMA precursor-1 is a precursor in the synthesis of prostate-specific membrane antigen (PSMA) ligands and fluorescent probes that have been used in the detection of PSMA in LNCaP and PC3 cells .
    PSMA precursor-1
  • HY-175248
    PSMA-DIM

    		PSMA Cancer
    PSMA-DIM is a dimeric PSMA ligand with a Kd of 37.09 nM for LNCaP cells. PSMA-DIM can be radiolabeled with [ 68Ga]Ga to form [ 68Ga]Ga-PSMA-DIM. [ 68Ga]Ga-PSMA-DIM can effectively distinguish between cells and animal models with different expression levels of PSMA. [ 68Ga]Ga-PSMA-DIM exhibits high LNCaP cells uptake and tumor uptake peak values. PSMA-DIM can be used for the study of prostate cancer (PCa) .
    PSMA-DIM
  • HY-149914
    WCA-814

    		Androgen Receptor Cancer
    WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell) .
    WCA-814
  • HY-106129
    Izonsteride

    LY 320236

    		 5 alpha Reductase Endocrinology Cancer
    Izonsteride (Compound LY320236) is an inhibitor of 5α-reductase (IC50 = 11.6 nM for type I; 7.37 nM for type II). LY320236 inhibits the activity of steroid 5α-reductase, preventing the conversion of testosterone (T) to dihydrotestosterone (DHT). LY320236 can significantly inhibit the growth of LNCaP tumors in thymic mice without exhibiting obvious host toxicity .
    Izonsteride
  • HY-163510
    AR/AR-V7-IN-1

    		Androgen Receptor Cancer
    AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
    AR/AR-V7-IN-1
  • HY-N1342
    Rocaglaol

    		Apoptosis Cancer
    Rocaglaol induces apoptosis and cell cycle arrest in LNCaP cells .
    Rocaglaol
  • HY-120581
    ML388

    		PGE synthase Cancer
    ML388 is a potent and selective hydroxyprostaglandin dehydrogenase (HPGD) inhibitor with an IC50 of 34 nM. ML388 induces PGE2 production in A549 cells and LNCaP prostate cancer cells .
    ML388
  • HY-118091A
    Bexlosteride

    LY300502

    		 5 alpha Reductase Cancer
    Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer .
    Bexlosteride
  • HY-144127
    AR antagonist 3

    		Androgen Receptor Cancer
    AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
    AR antagonist 3
  • HY-141830
    SYY-B029-2

    		Histone Acetyltransferase Cancer
    SYY-B029-2 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 of 1.4 nM. SYY-B029-2 cell growth of human mantle cell lymphoma (MCL) cell line MAVER-1 and human castration resistant prostate cancer cell line LNCaP clone FGC, with IC50 values of 15 nM and 13 nM, respectively .
    SYY-B029-2
  • HY-124585
    Y08060

    		Epigenetic Reader Domain Cancer
    Y08060 is a selective BET inhibitor. Y08060 inhibits the viability of C4-2B and LNCaP cell lines with IC50 values of 3.23 and 4.41 μM. Y08060 can suppress colony formation as well as AR expression in prostate cancer cell line. Y08060 can be studied in prostate cancer research .
    Y08060
  • HY-169282
    RGS2–Galpha-q PPI-IN-1

    		RGS Protein Cancer
    RGS2–Galpha-q interaction-IN-1 (Compound AJ-3) is an inhibitor of the RGS2-Galpha-q interaction. RGS2–Galpha-q interaction-IN-1 can inhibit the growth of cancer cell lines expressing RGS2 and exhibits anti-cell migration properties .
    RGS2–Galpha-q PPI-IN-1

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