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Results for "

GSPT1 degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (2) Antibody-Drug Conjugates (ADCs) (1) Apoptosis (12) Aquaporin (1) Bcl-2 Family (1) BCL6 (1) Btk (1) c-Myc (3) Casein Kinase (1) Caspase (3) CDK (5) DNA/RNA Synthesis (1) Drug Intermediate (3) E3 Ligase Ligand-Linker Conjugates (2) EGFR (1) Epigenetic Reader Domain (2) FLT3 (1) HDAC (1) Histone Methyltransferase (1) HSP (1) IKZF Family (4) JAK (1) Ligands for E3 Ligase (3) MDM-2/p53 (2) Molecular Glues (38) mTOR (1) NEKs (3) PARP (2) Pregnane X Receptor (PXR) (1) PROTAC Linkers (1) PROTACs (16) Reference Standards (1) Transmembrane Glycoprotein (1)
By Research Areas:	Cancer (64) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (3)

By Targets:

Androgen Receptor (2)

Antibody-Drug Conjugates (ADCs) (1)

Apoptosis (12)

Aquaporin (1)

Bcl-2 Family (1)

BCL6 (1)

Btk (1)

c-Myc (3)

Casein Kinase (1)

Caspase (3)

CDK (5)

DNA/RNA Synthesis (1)

Drug Intermediate (3)

E3 Ligase Ligand-Linker Conjugates (2)

EGFR (1)

Epigenetic Reader Domain (2)

FLT3 (1)

HDAC (1)

Histone Methyltransferase (1)

HSP (1)

IKZF Family (4)

JAK (1)

Ligands for E3 Ligase (3)

MDM-2/p53 (2)

Molecular Glues (38)

mTOR (1)

NEKs (3)

PARP (2)

Pregnane X Receptor (PXR) (1)

PROTAC Linkers (1)

PROTACs (16)

Reference Standards (1)

Transmembrane Glycoprotein (1)

By Research Areas:

Cancer (64)

Cardiovascular Disease (1)

Infection (1)

Inflammation/Immunology (3)

Inhibitors & Agonists

Screening Libraries

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-130800

Eragidomide 5+ Cited Publications CC-90009	Ligands for E3 Ligase Molecular Glues Apoptosis	Inflammation/Immunology Cancer
Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4 ^CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation .

HY-101488

CC-885 Maximum Cited Publications 18 Publications Verification	Molecular Glues Ligands for E3 Ligase	Cancer
CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of *GSPT1*, inhibiting protein translation.

HY-153356

MRT-2359	Molecular Glues Apoptosis	Inflammation/Immunology Cancer
MRT-2359 is an orally active and selective GSPT1 molecular glue degrader, with a DC₅₀ of 5 nM. MRT-2359 induces *CRBN*/GSPT1 ternary complex formation to drive CRBN- and degron-dependent proteasomal GSPT1 degradation, with selectivity for wild-type GSPT1 over the GSPT1^G575N mutant. MRT-2359 disrupts protein translation, induces ribosome stalling, downregulates MYC family proteins and their transcriptional output, reduces proliferation, and induces apoptosis in cancer cells. MRT-2359 can be used for the research of non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), neuroendocrine lung cancer, high grade neuroendocrine cancers, diffuse large B-cell lymphoma, prostate cancer, and MYC-driven solid tumors .

HY-145448

MC-VC-PABC-amide-PEG1-CH2-CC-885	E3 Ligase Ligand-Linker Conjugates	Cancer
MC-VC-PABC-amide-PEG1-CH2-CC-885 (compound I-1) is a neoDegrader-Linker conjugate, consists of the GSPT1 degrader/molecular glue CC-885 (HY-101488) and a linker. MC-VC-PABC-amide-PEG1-CH2-CC-885 can be conjugated to the antibody DAR3.7 that specifically targets CD56 to synthesize Antibody-Drug Conjugates (ADCs) .

HY-164202

ORM-5029	Antibody-Drug Conjugates (ADCs)	Cancer
ORM-5029 is a first-in-class human epidermal growth factor receptor 2 (HER2)-targeted antibody-drug conjugate (ADC) comprised of SMol006, a highly potent GSPT1 degrader, conjugated to Pertuzumab (HY-P9912). ORM-5029 exhibits robust efficacy across 14 HER2-positive breast cancer cell lines, with IC₅₀ values ranging from 0.3 to 14.4 nM.ORM-5029 demonstrates anti-tumor activity in the BT474 xenograft model. ORM-5029 can be used for study of breast cancer .

HY-132199

SJ6986 1 Publications Verification	Molecular Glues	Cancer
SJ6986 is a potent, selective and orally active *GSPT1/2* Molecular Glue degrader, with a DC₅₀ of 2.1 nM (D_max 99%) for GSPT1 .

HY-171792

BMS-986497 ORM-6151	Transmembrane Glycoprotein	Cancer
BMS-986497 (ORM-6151) is a CD33-targeting antibody-conjugated *GSPT1* degrader. BMS-986497 delivers the GSPT1 degrader SMol006 to CD33-expressing cells and induces GSPT1 protein degradation. BMS-986497 shows potential for research on acute myeloid leukemia (AML) .

HY-176444

CDK2 degrader 6	Molecular Glues CDK	Cancer
CDK2 degrader 6 is an orally active and potent CDK2 molecular glue degrader with a DC₅₀ of 46.5 nM. CDK2 degrader 6 binds to cereblon and CDK2 to induce ubiquitination and subsequent proteasomal degradation of CDK2. CDK2 degrader 6 modulates cell cycle in breast cancer cells. CDK2 degrader 6 reduces proliferation of breast cancer cells. CDK2 degrader 6 exhibits in vivo antitumor activity in gastric cancer mouse models. CDK2 degrader 6 can be used for the research of breast cancer, gastric cancer .

HY-155552

GSPT1 degrader-1	Apoptosis CDK Caspase	Cancer
GSPT1 degrader-1 is a highly selective degrader targeting *GSPT1. GSPT1* degrader-1 induces degradation via the ubiquitin-proteasome system. GSPT1 degrader-1 induces G₀/G₁ phase arrest, apoptosis (apoptosis) and inhibits proliferation in leukemia cells. GSPT1 degrader-1 reduces the levels of CDK6 and Cyclin B1, while increases the levels of activated caspase-3 and caspase-9 in leukemia cells. GSPT1 degrader-1 can be used in leukemia research .

HY-151902

SJ988497	PROTACs JAK	Cancer
SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL) .

HY-148837

GT19630	PROTACs c-Myc Casein Kinase	Infection Cardiovascular Disease Cancer
PROTAC c-Myc degrader-1 (Compound A153) is a multiple target protein degrader (PROTAC). PROTAC c-Myc degrader-1 effective degrades c-MYC, CK1α, *GSPT1* and IKZF1/2/3 proteins in a variety of tumor cells. PROTAC c-Myc degrader-1 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection (Pink: c-Myc ligand (HY-168685); Blue: E3 ligase ligand (HY-W093472); Black: linker (HY-W015808)) .

HY-130122

MG-277 1 Publications Verification	Molecular Glues PROTACs Apoptosis	Cancer
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, *GSPT1, with a DC₅₀* of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC₅₀s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .

HY-147158

ZXH-1-161	Molecular Glues	Cancer
ZXH-1-161 is a potent CRBN modulator that selectively induces the degradation of *GSPT1* in a CRBN-dependent manner. ZXH-1-161 can inhibit the proliferation of multiple myeloma cells and exhibits antitumor activity .

HY-150259

MDEG-541	PROTACs c-Myc	Cancer
MDEG-541 is a potent MYC-MAX degrader. MDEG-541 is a PROTAC that based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide (HY-14658). MDEG-541 shows antiproliferative activity. MDEG-541 decreases the expression of GSPT1, MYC, GSPT2, PLK1 protein .

HY-153803

GBD-9	PROTACs Molecular Glues Btk	Cancer
GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein *GSPT1. GBD-9 has both PROTAC* and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) . GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).

HY-150616

SJPYT-195	Pregnane X Receptor (PXR) Molecular Glues	Cancer
SJPYT-195 is a cytotoxic *GSPT1* degrader and can be used for PROTAC synthesis .

HY-175810

GSPT1 degrader-8	Molecular Glues	Cancer
GSPT1 degrader-8 is a potent and orally active G1 to S phase transition 1 (GSPT1) molecular glue degrader. GSPT1 degrader-8 induces GSPT1 degradation and inhibits tumor growth. GSPT1 degrader-8 can be used for the research of cancer, such as breast cancer .

HY-174238

GSPT1 degrader-7	Molecular Glues	Cancer
GSPT1 degrader-7 (Example 43) is a molecular glue degrader targeting *GSPT1. GSPT1* degrader-7 has an EC₅₀ of 0.2 nM in DF15 multiple myeloma cells. GSPT1 degrader-7 can be used in the study of cancer .

HY-156747

GSPT1 degrader-2	Molecular Glues DNA/RNA Synthesis	Cancer
GSPT1 degrader-2 (Compound 210) is a potent and orally active *GSPT1* molecular glue degrader (DC₅₀: < 30 nM). GSPT1 degrader-2 is an antitumor agent .

HY-161696

AN5777	Apoptosis	Cancer
AN5777 is a *GSPT1* degrader. AN5777 significantly reduces GSPT1 through the ubiquitin-proteasome system. AN5777 induces G1 block and Apoptosis. AN5777 has antitumor activity .

HY-136688

MI-389	PROTACs	Cancer
MI-389 is a PROTAC translation termination factor *GSPT1* degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4 ^CRBN E3 ligase .

HY-177761

GSPT1 degrader-15	Molecular Glues	Cancer
GSPT1 degrader-15 (Compound Lib-B-15O) is a potent and highly selective *GSPT1* molecular gel degrader, with a DC₅₀ of 154 nM. GSPT1 degrader-15 has almost no effect on the expression of other proteins. GSPT1 degrader-15 exhibits significant anti-proliferative activity against leukemia cells and lymphoma cells. GSPT1 degrader-15 can be used in leukemia and lymphoma research .

HY-168936

DP-15	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
DP-15 is the degrader for *GSPT1* and BRD4 with DC₅₀s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC₅₀ of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))

HY-170952

LYG-409	Molecular Glues	Cancer
LYG-409 is an orally active degrader of GSPT1. LYG-409 shows excellent anti-acute myeloid leukemia and prostate cancer in vivo with TGI of 94.34% and 104.49%, respectively. LYG-409 inhibits KG-1 cells mediated by the degradation of GSPT1 with an IC₅₀ of 9.50 nM, with a DC₅₀ of 7.87 nM in vitro .

HY-161101

MG degrader 1	PROTACs IKZF Family	Cancer
MG degrader 1 (Compd E14) is a PROTAC degrader of IKZF3, *GSPT1, and GSPT2* with an EC₅₀ value of 1.385 nM in MM.1S cells .

HY-159609

GSPT1 degrader-9	Molecular Glues	Cancer
GSPT1 degrader-9 (Compound F) is a cereblon-based molecular glue degrader for G1 to S phase transition protein 1 (GSPT1) that degrades GSPT1 with a rate of 95% (1 μM) GSPT1 and 86% (0.1 μM). GSPT1 degrader-9 inhibits the cell viability of HL-60 with an IC₅₀ of 9.2 nM .

HY-159610

GSPT1 degrader-10	Molecular Glues	Cancer
GSPT1 degrader-10 (compound A) is a cereblon-based molecular glue degrader of *GSPT1* with more than 95% degradation. GSPT1 degrader-8 inhibits cell viability in HL-60 cells with an IC₅₀ of 10 nM .

HY-162535

GSPT1 degrader-6	Molecular Glues	Cancer
GSPT1 degrader-6 (8) is a *GSPT1* molecule glue (DC₅₀ of 13 nM) .

HY-162534

GSPT1 degrader-5	Molecular Glues	Cancer
GSPT1 degrader-5 (4) is a *GSPT1* molecule glue (DC₅₀ of 144 nM) .

HY-W599279

ABS-752	Molecular Glues NEKs	Cancer
ABS-752 is a potent and orally active *GSPT1* and NEK7 molecular glue degrader. ABS-752 shows cytotoxicity. ABS-752 decreases the protein expression of GSPT1 and SALL4, NEK7. ABS-752 is a prodrug activated by the monoamine oxidase, VAP-1, to an aldehyde intermediate and subsequently to the active molecule, ABT-002 (HY-175283). ABS-752 has the potential for the research of hepatocellular carcinoma .

HY-177766

GSPT1 degrader-17	Molecular Glues Apoptosis	Cancer
GSPT1 degrader-17 (Compound 9q) is a potent and selective cereblon-based molecular glue degrader that targets G1 to S phase transition 1 (GSPT1). GSPT1 degrader-17 degrades GSPT1 in U937 cells with a DC₅₀ of 35 nM and Dmax of 81.65%. GSPT1 degrader-17 has a strong inhibitory effect on U937, MOLT-4 and MV4-11 cells with IC₅₀ values of 0.019, 0.006 and 0.027 μM. GSPT1 degrader-17 can induce cells apoptosis and G0/G1 phase arrest. GSPT1 degrader-17 can be used for the research of cancer, such as acute myeloid leukemia .

HY-177724

GSPT1 degrader-11	Molecular Glues	Cancer
GSPT1 degrader-11 is a CRBN-dependent G1 to S phase transition 1 (GSPT1) molecular glue degrader (DC₅₀ = 67.7 nM, D_max = 97%). GSPT1 degrader-11 can inhibit MDA-MB-231 CRBN-WT cells proliferation (IC₅₀ = 2.07 μM). GSPT1 degrader-11 can be used for the research of cancer .

HY-162533

GSPT1 degrader-4	Molecular Glues	Cancer
GSPT1 degrader-4 (3) is a *GSPT1* molecule glue (DC₅₀ of 25.4 nM), with an IC₅₀ of 39 nM for CAL51 proliferation .

HY-177765

GSPT1 degrader-16	Molecular Glues	Cancer
GSPT1 degrader-16 (Compound Lib-B-18J) is a potent and selective cereblon-based molecular glue degrader that targets G1 to S phase transition 1 (GSPT1). GSPT1 degrader-16 shows inhibitory effect to RS4;11, Molt4, and MM.1S cells with IC₅₀ values of 0.002, 0.26 and 0.37 μM. GSPT1 degrader-16 can be used for the research of cancer, such as acute lymphoblastic leukemi .

HY-157426

GSPT1 degrader-3	Epigenetic Reader Domain PROTACs	Cancer
GSPT1 degrader-3 (Pro-2) is a CRBN-based PROTAC degrader for BRD, with a DC₅₀ of 21.1 nM (4h) .

HY-175334

DHC-286	Molecular Glues	Cancer
DHC-286 is a molecular glue degrader targeting *GSPT1. DHC-286 recruits GSPT1* to the CRL4CRBN ubiquitin ligase complex, promoting GSPT1 ubiquitination and proteasomal degradation, inducing cytotoxicity. DHC-286 is promising for research of cancers such as acute myeloid leukemia .

HY-172770

KMG-1068	Molecular Glues	Cancer
KMG-1068 (Compound 4a), a molecular glue, is a *GSPT1/2* degrader. KMG-1068 effectively induces the CRBN-dependent degradation of GSPT1/2 by binding to the IMiD binding site on CRBN, facilitating the formation of a ternary complex with GSPT1/2. KMG-1068 is promising for research of cancers .

HY-177752

GSPT1 degrader-13	Molecular Glues	Cancer
GSPT1 degrader-13 is a selective molecular glue GSPT1 degrader. GSPT1 degrader-13 exhibits antiproliferative activity against cancer cells in a CRBN- and GSPT1-dependent manner. GSPT1 degrader-13 can be used for leukemia research .

HY-177753

GSPT1 degrader-14	Molecular Glues	Cancer
GSPT1 degrader-14 is a selective molecular glue GSPT1 degrader. GSPT1 degrader-14 exhibits antiproliferative activity against cancer cells in a CRBN- and GSPT1-dependent manner. GSPT1 degrader-14 can be used for leukemia research .

HY-170405

YB-3–17	PROTACs mTOR	Cancer
YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC₅₀=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC₅₀=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC₅₀ of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))

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 .

HY-177751

GSPT1 degrader-12	Molecular Glues	Cancer
GSPT1 degrader-12 is a selective molecular glue GSPT1 degrader. GSPT1 degrader-12 exhibits antiproliferative activity against cancer cells in a CRBN- and GSPT1-dependent manner. GSPT1 degrader-12 can be used for leukemia research .

HY-175040

PROTAC FLT-3 degrader 5	PROTACs Molecular Glues FLT3 IKZF Family	Cancer
PROTAC FLT-3 degrader 5 is a FLT3 PROTAC degrader (DC₅₀ = 1.2 nM). PROTAC FLT-3 degrader 5 functions as a molecular glue to degrade cereblon substrates GSPT1 and IKZF1/3. PROTAC FLT-3 degrader 5 exhibits antiproliferative activity against drug-resistant acute myeloid leukemia (AML) cells and is potentially useful in AML research. (Pink: FLT3/GSPT1/IKZF1/3 ligand: (HY-169374); Blue: Thalidomide: (HY-14658); Black: linker; Thalidomide + linker: (HY-W1123823)) .

HY-175283

ABT-002	Molecular Glues NEKs	Cancer
ABT-002 is a molecular glue degrader targeting *GSPT1* and NEK7. ABT-002 is the active metabolite of ABS-752 (HY-W599279). ABT-002 is promising for research of hepatocellular carcinoma (HCC) .

HY-177758

PROTAC HDAC6 degrader 8	PROTACs HDAC	Cancer
HDAC6 degrader-6 (Compound 11b) is a potent and selective HDAC6 PROTAC degrader with a DC₅₀ of 1.9 nM. HDAC6 degrader-6 has no effect on the protein levels of other HDAC family members and does not degrade IKZF1, IKZF3, and GSPT1. HDAC6 degrader-6 can be used to study multiple myeloma (Pink: HDAC6 ligand (HY-177776); Blue: CRBN ligand (HY-W998281); Black: Linker) .

HY-177750

TD-522	Molecular Glues Apoptosis	Cancer
TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC₅₀ of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research .

HY-174266

WB156	MDM-2/p53	Cancer
WB156 is a dual MDM2 and *GSPT1* degrader. WB156 can recruit CRBN (Cereblon, a substrate receptor of the E3 ubiquitin-ligase complex) to induce the ubiquitination-proteasome pathway-mediated degradation of MDM2 and GSPT1. WB156 is promising for research of cancers, such as leukemia .

HY-170820

XYD049	Molecular Glues Bcl-2 Family CDK EGFR HSP Androgen Receptor c-Myc	Cancer
XYD049 is a CRBN-based molecular glue degrader targeting *GSPT1, with a DC₅₀* of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and *GSPT1, thereby triggering CRBN- and proteasome-dependent degradation* of *GSPT1. By degrading* *GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, AR-V7, PSA* and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .

HY-177744

GSPT2 degrader-1	Molecular Glues	Cancer
GSPT2 degrader-1 (compound 619) is a selective molecular glue GSPT2 degrader targeting GSPT2. GSPT2 degrader-1 contains Thalidomide (HY-14658) and the linker of MDEG-541 (HY-150259). GSPT2 degrader-1 induces the degradation, but not GSPT1 or myelocytomatosis oncogene (MYC). GSPT2 degrader-1 can be used for research of gastrointestinal cancer .

HY-W1128213

IKZF2-degrader 2	Molecular Glues IKZF Family	Inflammation/Immunology Cancer
IKZF2-degrader 2 is a selective and orally active IKZF2 molecular glue degrader with DC₅₀ values of 0.5 nM and 1.8 nM in HiBit and FACS. The IKZF2-degrader 2 mediates the ubiquitination and degradation of target proteins by recruiting the CRL4-CRBN E3 ubiquitin ligase. IKZF2-degrader 2 displays moderate degradation against SALL4 with a DC₅₀ of 9 nM but does not induce any significant degradation towards IKZF1, IKZF3, CK1α and GSPT1. IKZF2-degrader 2 can be used for the study of cancer immunology .

Cat. No.	Product Name

HY-L935

Molecular Glue POI binding Fragment library

1039 compounds

POI (Protein of Interest) refers to the target protein, namely the disease-causing protein or key functional protein that undergoes degradation or functional modulation in molecular glue-mediated processes. The Molecular Glue POI Library consists of a series of fragments that can specifically bind to different types of POIs. As key components of molecular glues, these ligands form stable interactions with target proteins, laying the foundation for molecular glues to induce the interaction between POIs and E3 ubiquitin ligases. The covered POIs include various types such as cancer-associated GSPT1, androgen receptors, and abnormally aggregated proteins linked to neurodegenerative diseases.

This fragment library can be applied to the screening and optimization of targeted protein degraders. By screening ligands with high affinity and strong selectivity for specific POIs from the library, core structures can be identified to develop novel molecular glues. For instance, optimization of ligands targeting GSPT1 has yielded molecular glue degraders with enhanced degradation activity. Since many POIs are difficult to drug due to the lack of traditional small-molecule binding pockets, some ligands in the POI Ligand Library can modulate such POIs by inducing protein-protein interactions, thereby further expanding the scope of drug discovery for undruggable targets.

MCE has compiled a POI Fragment Library comprising thousands of POI fragments with molecular weights ranging from 150 to 400. This compound library can be widely applied in Molecular Glue research and development.

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