30

ARV-771

30 Publications Verification

Cat. No.: HY-100972

CAS No.: 1949837-12-0

Purity: 98.87%

Target:

PROTACs Epigenetic Reader Domain Apoptosis Ferroptosis c-Myc Androgen Receptor

Research Areas:

Cancer

ARV-771 is a BET PROTAC degrader, with K_d values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research .

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2

PROTAC AR-V7 degrader-1

2 Cited Publications

Cat. No.: HY-145479

CAS No.: 2767440-24-2

Purity: 98.19%

Target:

PROTACs Androgen Receptor

Research Areas:

Cancer

PROTAC AR-V7 degrader-1 is a selective AR-V7 degrader with a DC₅₀ of 0.32 μM. PROTAC AR-V7 degrader-1 inhibits cancer cell proliferation. PROTAC AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer .

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2

(R)-SKBG-1

2 Cited Publications

Cat. No.: HY-153918

CAS No.: 2955634-67-8

Purity: 99.50%

Target:

Androgen Receptor

Research Areas:

Cancer

(R)-SKBG-1 is a covalent inhibitor targeting the RNA binding protein NONO. (R)-SKBG-1 can reduce the expression of androgen receptor (AR) and its splice variants, inhibiting cancer cell proliferation. (R)-SKBG-1 inhibits androgen receptor expression with IC₅₀ of 3.1 μM and 5.5 μM for AR-FL mRNA and AR-V7 mRNA, respectively. (R)-SKBG-1 interferes with the gene regulatory network of cancer cells and inhibits cancer cell growth by stabilizing the interaction between NONO and mRNA. (R)-SKBG-1 can be used in the study of cancers related to NONO dysfunction, such as prostate cancer .

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1

MTX-23

1 Cited Publications

Cat. No.: HY-148771

CAS No.: 2488296-74-6

Purity: 99.79%

Synonyms: PROTAC AR-V7 degrader-2

Target:

PROTACs Androgen Receptor Apoptosis

Research Areas:

Cancer

MTX-23 is a PROTAC degrader targeting androgen receptor splice variant 7 (AR-V7) and full-length androgen receptor (AR-FL), with DC₅₀ values of 0.37 μM and 2 μM, respectively. MTX-23 binds to the DNA-binding domains of AR-V7 and AR-FL, recruits the VHL E3 ubiquitin ligase (E3 ubiquitin ligase) and induces their degradation. MTX-23 reduces the proliferation of prostate cancer cells, promotes their apoptosis (apoptosis), and also inhibits tumor growth in mouse models. MTX-23 can be used for the research of prostate cancer .

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EN1441

Cat. No.: HY-173626

CAS No.: 2196448-47-0

Target:

Androgen Receptor

Research Areas:

Cancer

EN1441 is a covalent degrader targeting the androgen receptor (AR) with an EC₅₀ value of 4.2 μM and its truncated variant AR-V7. EN1441 selectively and potently degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is promising for research of androgen-independent prostate cancers .

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Ralaniten triacetate

Cat. No.: HY-123875A

CAS No.: 1637573-04-6

Purity: 98.79%

Synonyms: EPI-506

Target:

Androgen Receptor

Research Areas:

Cancer

Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .

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SC912

Cat. No.: HY-161409

Target:

Androgen Receptor Apoptosis

Research Areas:

Cancer

SC912 is an AR-V7 inhibitor (IC₅₀ = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis .

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PROTAC AR/AR-V7 degrader-1

Cat. No.: HY-162412

CAS No.: 2841308-96-9

Target:

PROTACs Adrenergic Receptor Apoptosis

Research Areas:

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) .

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Ar-V7-IN-1

Cat. No.: HY-145709

CAS No.: 2230880-25-6

Purity: 98.02%

Target:

Androgen Receptor

Research Areas:

Cancer

Ar-V7-IN-1 is a potent inhibitor of Ar-V7. Ar-V7-IN-1 inhibits the transcriptional activity of androgen receptor (AR) and the secretion of prostate-specific antigen (PSA) with an eGFP IC₅₀ of 1232 nM and the PSA IC₅₀ of 1391 μM. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer .

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VPC-80051

Cat. No.: HY-126076A

CAS No.: 2410979-04-1

Target:

DNA/RNA Synthesis

Research Areas:

Cancer

VPC-80051 is an inhibitor of hnRNP A1 splicing activity. VPC-80051 directly interacts with hnRNP A1 RBD and reduces AR-V7 messenger levels in 22Rv1 CRPC cell line. VPC-80051 can be used in prostate cancer research .

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VPC-70063

Cat. No.: HY-147291

CAS No.: 13571-44-3

Purity: 99.92%

Target:

c-Myc PARP Apoptosis

Research Areas:

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 .

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