Epigenetic Reader Domain Degrader

Epigenetic Reader Domain Degraders (94):

Cat. No.	Product Name	Effect	Purity

HY-168236

PROTAC SMARCA2 degrader-28	Degrader
PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC₅₀ of 3 nM in HiBiT A549 cells. (Pink: Ligand for target protein (HY-168237); Black: Linker (HY-168238); Blue: Ligand for E3 ligase (HY-W087383))

HY-170900

SJ44236	Degrader
SJ44236 is the PROTAC degrader for BET that degrades BRD2 (DC₅₀ = 0.127 nM), BRD3 and BRD4. SJ44236 exhibits cytotoxicity in cell MV4-11 and HD-MB03 with IC₅₀s of 0.12 nM and 0.92 nM. SJ44236 downregulates the expression of c-Myc, upregulates the expression of p53. SJ44236 exhibits a good orally bioavailability of 45% in mice. (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W012935); Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 54 (HY-W890189))

HY-163877

PROTAC SMARCA2/4-degrader-19	Degrader
PROTAC SMARCA2/4-degrader-19 (Compound I-412) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-19 degrades SMARCA2 in MV411 and in A549 with DC₅₀ <100 nM, degrades SMARCA4 in MV411 with DC₅₀ <100 nM. (Pink: Ligand for Target Protein (HY-163949); Black: Linker (HY-W006635); Blue: Ligand for E3 Ligase (HY-125845))

HY-168448

dBAZ2	Degrader
dBAZ2 is a first-in-class BAZ2A and BAZ2B PROTAC degrader with DC₅₀ values of 180 nM and 250 nM for BAZ2A and BAZ2B, respectively. (Blue: E3 ligase ligand (VH 101, thiol (HY-47851); Black: linker (HY-168450); pink: target protein ligand (HY-168449)).

HY-160262

AR/BET protein degrader-1	Degrader
AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research.

HY-153820

PROTAC BRD4 Degrader-20	Degrader
PROTAC BRD4 Degrader-20 (compound 195) is an bifunctional compound and an degrader of BRD4.

HY-149948

PROTAC BRD3/BRD4-L degrader-2	Degrader
PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with K_i values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer.

HY-169278

PROTAC SMARCA2 degrader-26	Degrader
PROTAC SMARCA2 degrader-26 (compound 45) is a potent SMARCA2 PROTAC degrader. PROTAC SMARCA2 degrader-26 induces SMARCA2 and SMARCA4 degradation in VCaP cells with the percent degradation of 94% and 57% for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-26 shows antiproliferative activity.

HY-162744

PROTAC SMARCA2/4-degrader-31	Degrader
PROTAC SMARCA2/4-degrader-31 (Compound I-280) is a degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-31 degrades SMARCA2 in A549 with DC₅₀ <100 nM, degrades SMARCA4 in MV411 with DC₅₀ <100 nM. (Pink: Ligand for target protein (HY-163926); Black: Linker (HY-159682); Blue: Ligand for E3 ligase (HY-W382038)).

HY-169148

YT117R	Degrader
YT117R is a PROTAC degrader of FKBP12 and Pink: Target protein ligand: (HY-158301); Black: linker (HY-42776); Blue: E3 ligase ligand (HY-78695)).

HY-168936

DP-15	Degrader
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-169270

PROTAC SMARCA2 degrader-19	Degrader
PROTAC SMARCA2 degrader-19 (Compound 46) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 in cell A549 and MV411 with a DC₅₀ < 100 nM. PROTAC SMARCA2 degrader-19 degrades SMARCA4 in cell MV411 with a DC₅₀ > 1000 nM.

HY-169271

PROTAC SMARCA2 degrader-20	Degrader
PROTAC SMARCA2 degrader-20 (Compound I-40) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-20 has the potential for the research of cancer.

HY-143327

PROTAC BRD4 Degrader-16	Degrader
PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC₅₀ values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells.

HY-170808

PROTAC BRD4 Degrader-28	Degrader
PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-28 is promising for research of cancers (Pink: target protein ligand JQ-1 (carboxylic acid) (HY-78695); Black+ Blue: E3 ubiquitin ligase ligand-Linker conjugate Thalidomide-O-amido-C3-NH2 (HY-115560)).

HY-168453

dBAZ2B	Degrader
dBAZ2B is a BAZ2B PROTAC degrader, with a DC₅₀ of 19 nM. (Pink: BAZ2A/B ligand (HY-168449); Black: linker (HY-168450); Blue: CRBN Ligand (HY-125905))

HY-157426

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

HY-161883

JP-2-249	Degrader
JP-2-249 is a molecular glue that acts as a potent degrader of SMARCA2. JP-2-249 shows decreasing protein level of SMARCA2 in MV-4-11 cells at 1-10 μM.

HY-169269

PROTAC SMARCA2 degrader-18	Degrader
PROTAC SMARCA2 degrader-18 (Example144) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-18 has the potential for the research of non-small cell lung cancer (NSCLC).

HY-160527

BRD4 degrader-4	Degrader
BRD4 degrader-4 (Compound 1-f) is a BRD4 degrader. BRD4 degrader-4 can be used for the research of cancer and other bromodomain related diseases.

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