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Results for "

cereblon inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AAK1 (1) Akt (2) Aldose Reductase (1) Anaplastic lymphoma kinase (ALK) (3) Androgen Receptor (3) Apoptosis (24) Aurora Kinase (2) Autophagy (6) Bcl-2 Family (2) Btk (3) c-Met/HGFR (1) c-Myc (1) CaMK (1) CDK (7) E1/E2/E3 Enzyme (2) E3 Ligase Ligand-Linker Conjugates (6) EGFR (1) Epigenetic Reader Domain (4) FAK (1) Ferroptosis (1) FLT3 (1) Histone Acetyltransferase (1) Histone Methyltransferase (3) HSP (1) HuR (1) IKZF Family (2) IRAK (2) Isotope-Labeled Compounds (3) Itk (1) Kinesin (1) Ligands for E3 Ligase (13) Ligands for Target Protein for PROTAC (3) LIM Kinase (LIMK) (1) MDM-2/p53 (1) Molecular Glues (15) mTOR (1) NAMPT (1) NF-κB (2) p38 MAPK (1) PD-1/PD-L1 (1) PGE synthase (1) PROTAC Linkers (1) PROTACs (51) Ras (2) RIP kinase (1) Salt-inducible Kinase (SIK) (1) SARS-CoV (1) Sirtuin (1) STAT (1) ULK (1) YAP (1)
By Research Areas:	Cancer (76) Infection (1) Inflammation/Immunology (14) Metabolic Disease (1)
Click Chemistry:	Azide (3) Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-143715

Cereblon inhibitor 1	Ligands for E3 Ligase	Cancer
Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.

HY-153661

Cereblon inhibitor 2	Ligands for E3 Ligase Autophagy Apoptosis	Cancer
Cereblon inhibitor 2 (compound 8) is a *Cereblon* inhibitor useful in solid tumor research, especially breast cancer .

HY-W145436

Thalidomide-Piperazine 5-fluoride hydrochloride	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
Thalidomide-Piperazine 5-fluoride hydrochloride is a derivative of cereblon (CRBN) inhibitor Thalidomide (HY-14658), which can be used as ligands for E3 ubiquitin ligase (Ligands for E3 Ligase) for PROTACs Synthesis .

HY-148063

DB0614	PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK	Metabolic Disease
DB0614 is a PROTAC based on *Cereblon* ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))

HY-111870

PROTAC RIPK degrader-6	PROTACs RIP kinase	Cancer
PROTAC RIPK degrader-6 (example 1) is a *Cereblon*-based PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder .

HY-100507

Avadomide 5+ Cited Publications CC 122	E1/E2/E3 Enzyme Apoptosis Molecular Glues NF-κB	Inflammation/Immunology Cancer
Avadomide is an orally active *cereblon* modulator. Avadomide modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide exhibits potent antitumor and immunomodulatory activities .

HY-157511

Thalidomide-O-C5-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-O-C5-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C5-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C5-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-157510

Thalidomide-O-C3-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-O-C3-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C3-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C3-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-157515

Thalidomide 4'-ether-PEG2-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide 4'-ether-PEG2-azide is a click chemistry modified cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide 4'-ether-PEG2-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkynyl groups. Thalidomide 4'-ether-PEG2-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-158760

PROTAC IRAK4 degrader-11	PROTACs IRAK	Cancer
PROTAC IRAK4 degrader-11 (compound 15) is PROTAC based on Cereblon ligand, and induces the degradation of IRAK4 with maximum degradation of 96.25% and the DC₅₀ of 2.29 nM in HEK293 cells(Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker；Pink: IRAK4 inhibitor) .

HY-100507A

Avadomide hydrochloride CC 122 hydrochloride	E1/E2/E3 Enzyme Apoptosis Molecular Glues NF-κB	Inflammation/Immunology Cancer
Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active *cereblon* modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities .

HY-101488

CC-885 10+ Cited Publications	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-115568

BETd-246 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for *Cereblon* and BET, exhibiting superior selectivity, potency and antitumor activity .

HY-160506

PRO-6E	PROTACs c-Met/HGFR Apoptosis	Cancer
PRO-6E is an oral active PROTAC based on *Cereblon* ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .

HY-161574

LLC0424	PROTACs Histone Methyltransferase	Cancer
LLC0424 is a potent and selective *cereblon*-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC₅₀ of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .

HY-138946

XY028-140	CDK PROTACs	Cancer
XY028-140 is a PROTAC connected by ligands for *Cereblon* and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells .

HY-125876

PROTAC Bcl2 degrader-1 1 Publications Verification	PROTACs Bcl-2 Family	Cancer
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on *Cereblon* ligand, which potently and selectively induces the degradation of Bcl-2 (IC₅₀, 4.94 μM; DC₅₀, 3.0 μM) and Mcl-1 (IC₅₀, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker；Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).

HY-156111

ARD-1676	PROTACs Androgen Receptor	Cancer
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .

HY-130612

PROTAC BRD2/BRD4 degrader-1	Epigenetic Reader Domain PROTACs	Cancer
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for *Cereblon* and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .

HY-131717A

Thalidomide-NH-CH2-COOH TFA	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-NH-CH2-COOH TFA is a ligand-linker conjugate for the E3 ligase Cereblon (CRBN). Thalidomide-NH-CH2-COOH TFA can be conjugated to multi-targeted kinase inhibitors to transform them into selective degraders .

HY-159015

SIAIS630120-NC	PROTACs	Cancer
SIAIS630120-NC is a negative control for NAMPT (nicotinamide phosphoribosyltransferase) degrader SIAIS630120 (Sturcture Note:(Blue: Cereblon ligand Thalidomide (HY-14658) analogue (HY-138793), Black: linker；Pink: Nampt inhibitor FK866 (HY-50876)) .

HY-159016

SIAIS630121-NC	PROTACs	Cancer
SIAIS630121-NC is a negative control for NAMPT (nicotinamide phosphoribosyltransferase) degrader SIAIS630121(Sturcture Note:(Blue: Cereblon ligand Thalidomide (HY-14658) analogue (HY-138793), Black: linker；Pink: Nampt inhibitor FK866 (HY-50876)) .

HY-125835

CP-10 1 Publications Verification	PROTACs CDK	Cancer
CP-10 is a PROTAC connected by ligands for *Cereblon* and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC₅₀=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6 .

HY-125877

PROTAC Mcl1 degrader-1 1 Publications Verification	PROTACs Bcl-2 Family	Cancer
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on *Cereblon* ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC₅₀ of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC₅₀ of 0.54 μM .

HY-153821

PROTAC KRAS G12C degrader-2	Ras PROTACs	Cancer
PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .

HY-153803

GBD-9	PROTACs Molecular Glues Btk	Cancer
GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth .

HY-14658

Thalidomide 15+ Cited Publications	Ligands for E3 Ligase Autophagy Apoptosis Molecular Glues	Inflammation/Immunology Cancer
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a K_d of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

HY-153386

CPD-1224	Anaplastic lymphoma kinase (ALK)	Cancer
CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .

HY-14658S

Thalidomide-d4	Molecular Glues Ligands for E3 Ligase Autophagy Apoptosis	Inflammation/Immunology Cancer
Thalidomide-d₄ is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties[1][2].

HY-133120A

INY-03-041 trihydrochloride 1 Publications Verification	PROTACs Akt	Cancer
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, *Cereblon* ligand). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

HY-133120

INY-03-041 1 Publications Verification	PROTACs Akt	Cancer
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, *Cereblon* ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

HY-168614

MGD-4	IKZF Family	Cancer
MGD-4 is an orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC₅₀=67.2 nM), IKZF2 (DC₅₀=918.2 nM), and IKZF3 (DC₅₀=95.8 nM) in a dose-dependent manner. MGD-4 effectively inhibits the growth of multiple myeloma .

HY-110167

TFC 007	PGE synthase Ligands for Target Protein for PROTAC	Cancer
TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC₅₀ value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon) .

HY-168586

PROTAC IRAK4 degrader-12	PROTACs IRAK	Cancer
PROTAC IRAK4 degrader-12 is a PROTAC based on Cereblon ligand, inducing a maximum degradation rate of IRAK4 of 108.46% in K562 cells with an IC₅₀ value of 4.87 nM ( Structure Note: Pink, IRAK4 inhibitor (HY-168611); Blue, E3 (HY-W733885); Black, linker (HY-168613)) .

HY-162464

MPD2	PROTACs SARS-CoV	Infection
MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the main protease of SARS-CoV-2. MPD2 effectively reduced MPro protein levels in 293T cells in a time-dependent manner (DC₅₀=296 nM). MPD2 exhibited potent antiviral activity against multiple SARS-CoV-2 strains and had enhanced potency against Nirmatrelvir (HY-138687) resistant strains. MPD2 provides a new direction for antiviral drug development against SARS-CoV-2 and other emerging coronavirus pathogens (Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker (HY-W275882)；Red: SARS-CoV-2 MPro Inhibitor MP18 (HY-158763)) .

HY-154984

JET-209	Histone Acetyltransferase PROTACs	Cancer
JET-209 is a potent PROTAC CBP/p300 degrader, with DC₅₀ values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 contains Lenalidomide (HY-A0003) (the cereblon ligand), a linker and GNE-207 (HY-120028) (bromodomain Inhibitor). JET-209 is used for cancer research .

HY-130854

Thalidomide-NH-C6-NH-Boc	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A) .

HY-114407

TD-428	PROTACs Epigenetic Reader Domain	Cancer
TD-428 is a PROTAC connected by ligands for *Cereblon* and BRD4. TD-428 is a highly specific BRD4 degrader with a DC₅₀ of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .

HY-163759

HuR degrader 2	Molecular Glues HuR	Cancer
HuR degrader 2 (Compound 3) is a molecule glue, which targets RNA-binding protein Hu antigen R (HuR) and degrades 30% HuR at 0.1 μM. HuR degrader 2 inhibits the proliferation of cancer cell Colo-205, with IC₅₀≤200 nM. HuR degrader 2 exhibits a high affinity with cereblon, with an HTRF ratio < 0.02 .

HY-14658R

Thalidomide (Standard)	Ligands for E3 Ligase Autophagy Apoptosis	Inflammation/Immunology Cancer
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a K_d of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

HY-130665

TL12-186 1 Publications Verification	PROTACs CDK	Cancer
TL12-186 is a *Cereblon*-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC₅₀=73 nM) and CDK9/cyclin T1 (IC₅₀=55 nM) .

HY-162537

LYP-8	PROTACs NAMPT	Cancer
LYP-8 is a potent and effective NAMPT degrader with maximum degradation of 97% at 0.5 μM in SKOV-3 cells. LYP-8 shows anti-cancer activity in vivo and in vitro(Sturcture Note:(Blue: Cereblon ligand (HY-112078), Black: linker (HY-128801)；Pink: Nampt inhibitor Nampt-IN-11 (HY-158689)) .

HY-162589

Lw13	PROTACs HSP Apoptosis	Cancer
Lw13 is a Hsp90-targeting PROTAC and achieves maximum degradation at a concentration of 0.05 μM in Siha cells. Lw13 induces cell apoptosis and exhibits potent anti-tumor activity both in vitro and in vivo(Sturcture Note:(Blue: Cereblon ligand (HY-A0003), Black: linker；Pink: Hsp90 inhibitor SNX-5422 (HY-10213)) .

HY-161450

LHF418	PROTACs Ras	Cancer
LHF418 is an effective SOS1 PROTAC degrader with a DC₅₀ value of 209.4 nM in A549 cells. LHF418 can effectively inhibit RAS signaling and colony formation in KRAS-driven cancer cells. (Structural note: (Blue: Cereblon ligand (HY-A0003), Black: linker; Pink: SOS1 binder SOS1 Ligand intermediate-3 (HY-161452)) .

HY-111546

BI-3663 1 Publications Verification	PROTACs FAK	Cancer
BI-3663 is a highly selective PTK2/FAK PROTAC (DC₅₀=30 nM), with *Cereblon* ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC₅₀ of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker . Anti-cancer activity .

HY-44103

Desmethyl-QCA276 PROTAC BRD4-binding moiety 4	Ligands for Target Protein for PROTAC	Cancer
Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC₅₀ of 10 nM, and with a K_i of 2.3 nM . Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-123919

TL13-112 1 Publications Verification	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC₅₀ value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC₅₀ values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib?(HY-15656) and the *Cereblon* ligand of Pomalidomide (HY-10984) .

HY-139039

BSJ-4-116	PROTACs CDK	Cancer
BSJ-4-116 is a PROTAC connected by ligands for *Cereblon* and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC₅₀ of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162) .

HY-141512

JB170 1 Publications Verification	PROTACs Aurora Kinase	Cancer
JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC₅₀=28 nM) by linking Alisertib, to the *Cereblon*-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC₅₀=193 nM) over AURORA-B (EC₅₀=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase .

HY-122582

TL13-12	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC₅₀ value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC₅₀ values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the *Cereblon* ligand of Pomalidomide (HY-10984) .

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library

65 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.

Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).

MCE carefully prepared a unique collection of 65 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

Cat. No.	Product Name	Chemical Structure

HY-A0003S

Lenalidomide-d5

Lenalidomide-d₅ is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].

HY-14658S

Thalidomide-d4
Thalidomide-d₄ is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties[1][2].

HY-A0003S2

Lenalidomide-13C5,15N

Lenalidomide- ¹³C₅, ¹⁵N is ¹⁵N and ¹³C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .

HY-A0003S3

Lenalidomide-d4

Lenalidomide-d₄ (CC-5013-d₄) is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .

Cat. No.	Product Name		Classification

HY-157511

Thalidomide-O-C5-azide		Azide
Thalidomide-O-C5-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C5-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C5-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-157510

Thalidomide-O-C3-azide		Azide
Thalidomide-O-C3-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C3-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C3-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-157515

Thalidomide 4'-ether-PEG2-azide		Azide
Thalidomide 4'-ether-PEG2-azide is a click chemistry modified cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide 4'-ether-PEG2-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkynyl groups. Thalidomide 4'-ether-PEG2-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .

HY-107453

SirReal1-O-propargyl PROTAC Sirt2-binding moiety 1		Alkynes
SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC₅₀ of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2 . SirReal1-O-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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