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CDK2 degrader 1

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By Targets:	CDK (9) Caspase (1) E3 Ligase Ligand-Linker Conjugates (1) FLT3 (1) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (1) PROTAC Linkers (1) PROTACs (8)
By Research Areas:	Cancer (12)

Targets Recommended: CDK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-163814

**CDK2 degrader 1**	Molecular Glues CDK	Cancer
CDK2 degrader 1 (Compound 3) is a selective CDK2 molecular glue degrader with a D_max (CDK2) of > 80% and a K_i (CRBN) > 1 μM. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers .

HY-130709

PROTAC CDK2/9 Degrader-1	PROTACs CDK	Cancer
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for *CDK2* (DC₅₀=62 nM) and CDK9 (DC₅₀=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC₅₀=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand .

HY-168057

PROTAC CDK2 Degrader-1	PROTACs CDK	Cancer
PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader for cyclin-dependent kinase 2 (CDK2). PROTAC CDK2 Degrader-1 inhibits the phosphorylation of RB protein in CDK2 dependent cell line OVCAR3 with an IC₅₀ of 100-500 nM .

HY-130713

Thalidomide-C2-amido-C2-COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-C2-amido-C2-COOH contains a CRBN ligand and a linker for recruiting E3 ubiquitin ligases. Thalidomide-C2-amido-C2-COOH can be used to design and synthesize PROTAC CDK2/9 Degrader-1 (HY-130709). PROTAC CDK2/9 Degrader-1 is applicable to prostate cancer-related research .

HY-179688

PROTAC CDK2/4 Degrader-1	PROTACs CDK	Cancer
PROTAC CDK2/4 Degrader-1 (Compound 5) is a CDK2/4 PROTAC degrader, with its DC₅₀ values for CDK2 and CDK4 both ≤ 10 nM. PROTAC CDK2/4 Degrader-1 exhibits excellent inhibitory activity against cell proliferation in OVCAR3 and T47D cells. PROTAC CDK2/4 Degrader-1 can be used for research on breast cancer and ovarian cancer .

HY-186132

PROTAC CDK2-pRb degrader-1	PROTACs CDK	Cancer
PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of *CDK2. PROTAC CDK2-pRb* degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of *CDK2. PROTAC CDK2-pRb* degrader-1 exhibits significant activity against human cells (with EC₅₀ values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer) .

HY-171826

PROTAC CDK2/4/6 Degrader-1	CDK PROTACs	Cancer
PROTAC CDK2/4/6 Degrader-1 is an orally active *CDK2/CDK4/CDK6* PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research .

HY-161708

PROTAC FLT3/CDKs degrader-1	PROTACs CDK FLT3	Cancer
PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC₅₀ is 18.73 nM for *CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1* induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC₅₀s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))

HY-130712

NH2-C2-amido-C2-Boc	PROTAC Linkers	Cancer
NH2-C2-amido-C2-Boc is a PROTAC linker, which refers to the alkyl/ether composition. NH2-C5-NH-Boc can be used in the synthesis of a series of PROTACs, such as the PROTAC CDK2/9 Degrader-1 (HY-130709) .

HY-W1047040

CDK2/4 ligand 1	Ligands for Target Protein for PROTAC CDK	Cancer
CDK2/4 ligand 1 is a ligand for target protein for PROTACs, which targets *CDK2/4. CDK2/4 ligand 1 can be used for synthesis of PROTAC CDK2/4 Degrader-1* (HY-179688) .

HY-185121

*PROTAC CDK2/4/6 Degrader-2*	PROTACs CDK Caspase	Cancer
PROTAC CDK2/4/6 Degrader-2 is a *CDK2/4/6* PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades *CDK2/4/6* and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research .

HY-W883326

CRBN ligand-902	Ligands for E3 Ligase	Others
CRBN ligand-902 is a CRBN E3 ligase ligand that can be used for synthesis of PROTAC CDK2/4 Degrader-1 (HY-179688) .

HY-181134

PROTAC HMGCR Degrader-2	PROTACs	Cancer
PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader with an IC₅₀ value of 0.25 μM. PROTAC degrades HMGCR-2 in Insig-silenced HepG2 cells with a DC₅₀ of 0.12 μM. PROTAC HMGCR Degrader-2 takes PROTAC HMGCR Degrader-1 (HY-171823) as the oral prodrug. PROTAC HMGCR Degrader-2 degrades HMGCR by the VHL-dependent ubiquitin-proteasome system and reduces cellular cholesterol in HepG2 cells. PROTAC CDK2/4/6 Degrader-2 can be used for hyperlipidemia research .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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CDK2 degrader 1

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