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22RV1

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54

Inhibitors & Agonists

1

Inhibitory Antibodies

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149495
    CP-07

    		PROTACs CDK Cancer
    CP-07 is a potent and selective PROTACCDK9 degrader (DC50: 43 nM). CP-07 inhibits 22RV1 cell proliferation (IC50: 62 nM) and colony formation by down-regulating Mcl-1 and c-Myc. CP-07 inhibits 22RV1 xenograft tumor growth. CP-07 can be used for research of prostate cancer .
    CP-07
  • 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-143235
    BRD4 Inhibitor-15

    		Epigenetic Reader Domain Apoptosis Bcl-2 Family Caspase c-Myc Cancer
    BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
    BRD4 Inhibitor-15
  • HY-150268
    BET-IN-16

    		Epigenetic Reader Domain Cancer
    BET-IN-16 (Comp I) is a BET inhibitor. BET-IN-16 shows anticancer activity. BET-IN-16 inhibits prostate cancer cell growth, with IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively .
    BET-IN-16
  • HY-163281
    FSY-OSO2F

    		Fluorescent Dye Cancer
    FSY-OSO2F shows an uptake in MCF-7 cells through the regulation of L-Tyr, ASC, and ASC2 transporters. FSY-OSO2F can be used as a PET tracer, when labeled with 18F, and exhibits good uptake and good contrast in MCF-7 and 22Rv1 subcutaneous tumors .
    FSY-OSO2F
  • 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-142772
    Y08284

    		Epigenetic Reader Domain Cancer
    Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity .
    Y08284
  • HY-158432
    GT-653

    		Histone Demethylase PROTACs Cancer
    GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
    GT-653
  • 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-121588
    IMTPPE

    		Adrenergic Receptor Cancer
    IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors .
    IMTPPE
  • HY-161769
    HL435

    		PROTACs Epigenetic Reader Domain Apoptosis Cancer
    HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
    HL435
  • 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-133020
    ARD-266

    		PROTACs Androgen Receptor Cancer
    ARD-266 is a highly potent and von Hippel-Lindau 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 . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-266
  • HY-145479
    PROTAC AR-V7 degrader-1

    		PROTACs Androgen Receptor Cancer
    PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM .
    PROTAC AR-V7 degrader-1
  • HY-133044
    Boc-Pip-alkyne-Ph-COOH

    		PROTAC Linkers Cancer
    Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . Boc-Pip-alkyne-Ph-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Boc-Pip-alkyne-Ph-COOH
  • HY-160777
    VNPP433-3β

    Galeterone 3β-imidazole

    		 Androgen Receptor MNK Cancer
    VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
    VNPP433-3β
  • HY-121522
    SD-70

    		Histone Demethylase Cancer
    SD-70 is an inhibitor for histone demethylase JMJD2C and exhibits antitumor efficacy. SD-70 inhibits viability of cancer cells CWR22Rv1 (9% cell survival at 10 μM), PC3 (14% cell survival at 2 μM) and DU145 (26% cell survival at 2 μM) .
    SD-70
  • HY-160260
    EP300/CBP-IN-1

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC50s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells .
    EP300/CBP-IN-1
  • HY-163611
    XY039

    		ROR Cancer
    XY039 (compound 13e) is a RORγ inverse agonist with the IC50 of 0.55 μM. XY039 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
    XY039
  • HY-163612
    XY077

    		ROR Apoptosis Cancer
    XY077 (compound 14a) is a RORγ inverse agonist with the IC50 of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
    XY077
  • HY-146573
    AKR1C3-IN-6

    		Others Cancer
    AKR1C3-IN-6 (Compound 1) is a potent, selective AKR1C3 inhibitor with IC50 values of 0.31 μM and 73.23 μM against AKR1C3 and AKR1C2, respectively. AKR1C3-IN-6 shows antitumor activity .
    AKR1C3-IN-6
  • HY-146574
    AKR1C3-IN-7

    		Others Cancer
    AKR1C3-IN-7 (Compound 13) is a potent, selective AKR1C3 inhibitor with an IC50 of 0.19 μM. AKR1C3-IN-7 shows antitumor activity .
    AKR1C3-IN-7
  • HY-146575
    AKR1C3-IN-8

    		Others Cancer
    AKR1C3-IN-8 (Compound 5) is a potent, selective AKR1C3 inhibitor with an IC50 of 0.069 μM. AKR1C3-IN-8 shows antitumor activity .
    AKR1C3-IN-8
  • HY-153918
    (R)-SKBG-1

    		Androgen Receptor Cancer
    (R)-SKBG-1 is an RNA-binding protein NONO inhibitor. (R)-SKBG-1 suppresses androgen receptor expression with IC50s of 3.1 μM and 5.5 μM against AR-FL mRNA and AR-V7 mRNA, respectively .
    (R)-SKBG-1
  • HY-162412
    PROTAC AR/AR-V7 degrader-1

    		PROTACs Adrenergic Receptor Apoptosis Cancer
    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) .
    PROTAC AR/AR-V7 degrader-1
  • HY-158433
    KDM5B ligand 2

    		Ligands for Target Protein for PROTAC Histone Demethylase Cancer
    KDM5B ligand 2 is the ligand for target protein KDM5B. KDM5B ligand 2 is utilized for synthesis of KDM5B PROTAC GT-653 (HY-158432) .
    KDM5B ligand 2
  • HY-164005
    CBP/EP300 bromodomain receptor-IN-1

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CBP/EP300 bromodomain receptor-IN-1 (Compound 10) is an inhibitor for CBP/EP300 bromodomain receptor, which binds to proteins having a bromodomain in nanomolar level .
    CBP/EP300 bromodomain receptor-IN-1
  • HY-103245
    Cl-4AS-1

    		Androgen Receptor Cancer
    Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively) .
    Cl-4AS-1
  • HY-149297
    PSMA-IN-1

    		PSMA Cancer
    PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. PSMA-IN-1 inhibits tumor growth with high selectivity and specificity in PSMA+ xenograft models. PSMA-IN-1 is a NIR probe (λEX: 620 nm; λEM: 670 nm) used for tumor disappearance. PSMA-IN-1 can be used for research on prostate cancer .
    PSMA-IN-1
  • HY-155571
    MDM2/XIAP-IN-3

    		MDM-2/p53 IAP Cancer
    MDM2/XIAP-IN-3 (compound 3e) is a dual MDM2/XIAP inhibitor. MDM2/XIAP-IN-3 reduces MDM2 and XIAP protein levels and increases p53 expression, thereby inhibiting cancer cell growth and causing cell death .
    MDM2/XIAP-IN-3
  • HY-163192
    W6134

    		ROR Cancer
    W6134 is highly potent and selective RORγ covalent inhibitor with IC50 of 0.21 μM. W6134 exhibits superior activity ini nhibiting the proliferation and colony formation and inducing apoptosis. W6134 can be used for the research of cancer .
    W6134
  • HY-112659
    Lin28-let-7 antagonist 1

    		Others Neurological Disease Cancer
    Lin28-let-7 antagonist 1 (compound 1632) is a potent antagonist of Lin28/pre-let-7 interaction. Lin28-let-7 antagonist 1 inhibits Lin28A binding to pre-let-7a-2, with an IC50 of 8 μM. Lin28-let-7 antagonist 1 inhibits proliferation in human cancer cells .
    Lin28-let-7 antagonist 1
  • HY-P99762
    Obrindatamab

    MGD009

    		 CD3 Cancer
    Obrindatamab is a humanized anti-B7-H3/CD3 bispecific antibody. Obrindatamab binds to B7-H3 and CD3, thereby mediating redirected cytotoxic T-lymphocyte (CTL) activity against B7-H3-expressing cancer cells. Obrindatamab can be used in research of cancer .
    Obrindatamab
  • HY-142743
    Y08175

    		Epigenetic Reader Domain Cancer
    Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer .
    Y08175
  • HY-149927
    Antitumor agent-91

    		Others Cancer
    Antitumor agent-91 is a cyclic phosphate ester derivative with anticancer and anti-proliferative activities. Antitumor agent-91 has potential application in human castration resistant prostate cancer and pancreatic cancer .
    Antitumor agent-91
  • HY-161369
    CBPD-268

    		PROTACs Histone Acetyltransferase Cancer
    CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .
    CBPD-268
  • HY-163609
    PROTAC AKR1C3 degrader-1

    		PROTACs Aldose Reductase Cancer
    PROTAC AKR1C3 degrader-1 (compound 5) is a potent AKR1C3 PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)) .
    PROTAC AKR1C3 degrader-1
  • HY-122108
    Ilicicolin A

    LL-Z 1272-alpha

    		 Apoptosis Cancer
    Ilicicolin A is a potent anticancer agent. Ilicicolin A induces apoptosis. Ilicicolin A inhibits cell growth and colony formation. Ilicicolin A shows antitumor activity. Ilicicolin A has the potential for the research of prostate cancer .
    Ilicicolin A
  • HY-16187
    EL-102

    		HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer .
    EL-102
  • HY-149298
    PSMA-IN-2

    		PSMA Cancer
    PSMA-IN-2 is an inhibitor of PSMA with a Ki value of 1.07 nM. PSMA-IN-2 displays favorable in vivo NIR imaging (λEM = 1088 nm, λex = 808 nm), and can be used for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice .
    PSMA-IN-2
  • HY-146445
    P300 bromodomain-IN-1

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC50 of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells .
    P300 bromodomain-IN-1
  • HY-143317
    XY153

    		Epigenetic Reader Domain Cancer
    XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
    XY153
  • HY-151385
    VVD-118313

    		JAK STAT IFNAR Interleukin Related Cancer
    VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer . VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    VVD-118313
  • HY-161770
    HL389

    		Ligands for E3 Ligase Cancer
    HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769) .
    HL389
  • HY-161773
    HL389-NHC2-PEG3-C2NH

    		E3 Ligase Ligand-Linker Conjugates Cancer
    HL389-NHC2-PEG3-C2NH inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389-NHC2-PEG3-C2NH can be utilized as a conjugate of an E3 ligase ligand and a linker, for the synthesis of PROTAC degrader HL435 (HY-161769) .
    HL389-NHC2-PEG3-C2NH
  • HY-162568
    7-tert-Butylfascaplysin

    		DNA Stain Cancer
    7-tert-Butylfascaplysin (7-TB) is a derivative of Fascaplysin (HY-112328), that can be isolated from Fascaplysinopsis sp.. 7-tert-Butylfascaplysin induces replication stress, leads to toxic DNA double-strand breaks and apoptosis-like cell death, and thus exhibits cytotoxicity in cancer cells in nanomolar levels. 7-tert-Butylfascaplysin exhibits DNA intercalating activity with EC50 of 3.2 μM .
    7-tert-Butylfascaplysin
  • HY-162706
    BSJ-5-63

    		CDK Cancer
    BSJ-5-63 is a potent CDK12, CDK7, CDK9 degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer .
    BSJ-5-63
  • HY-151266
    AR antagonist 4

    		Androgen Receptor Cancer
    AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM .
    AR antagonist 4
  • HY-124056
    AZ10397767

    		CXCR Cancer
    AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
    AZ10397767
  • HY-108986
    JFD00244

    		Sirtuin SARS-CoV Cancer
    JFD00244 is a sirtuin 2 (SIRT2) inhibitor, with anti-tumor effect. JFD00244 is also a Nsp-16 inhibitor against SARS-CoV-2 .
    JFD00244

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