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BRDT-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Epigenetic Reader Domain (12)
By Research Areas:	Cancer (5) Endocrinology (5) Inflammation/Immunology (1)

Inhibitors & Agonists

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-136571

GSK046 3 Publications Verification iBET-BD2	Epigenetic Reader Domain	Inflammation/Immunology
GSK046 (iBET-BD2), a chemical probe, is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC₅₀s of 264 nM (BRD2 *BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2),* respectively. GSK046 has immunomodulatory activity .

HY-131061

BET bromodomain inhibitor 1	Epigenetic Reader Domain	Cancer
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC₅₀ of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (K_d values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .

HY-138563

GSK973	Epigenetic Reader Domain	Cancer
GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the *BD2s* (second bromodomains) of the BET family, with a pIC₅₀ of 7.8 and a pK_d of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC₅₀=7.4~7.8; pK_d=8.3~8.5) .

HY-183248

*BRDT-IN-2*	Epigenetic Reader Domain	Cancer
BRDT-IN-2 is a *BRDT-BD1*-preferring inhibitor (K_i=10 μM) with higher affinity for *BRDT-BD1* than BRD4-BD1. BRDT-IN-2 preferentially binds *BRDT-BD1* without direct interaction with *BRDT-BD1’s Arg54 residue. BRDT-IN-2* binds BRD4-BD1 with lower affinity via structured water molecule displacement in its binding pocket. BRDT-IN-2 can be used for the research of multiple myeloma .

HY-177143

CDD-1498	Epigenetic Reader Domain	Endocrinology
CDD-1498 (Compound 12) is a potent inhibitor of *BRDT-BD2. CDD-1498 has an IC₅₀* of 978 nM against BRDT-BD2. CDD-1498 can be studied in research on nonhormonal contraceptive agent .

HY-177145

CDD-1132	Epigenetic Reader Domain	Endocrinology
CDD-1132 (Compound 8) is a potent inhibitor of *BRDT-BD2. CDD-1132 has an IC₅₀* of 13 nM against BRDT-BD2. CDD-1132 can be studied in research on nonhormonal contraceptive agent .

HY-177144

CDD-1128	Epigenetic Reader Domain	Endocrinology
CDD-1128 (Compound 11) is a potent inhibitor of *BRDT-BD2. CDD-1128 has an IC₅₀* of 521 nM against BRDT-BD2. CDD-1128 can be studied in research on nonhormonal contraceptive agent .

HY-177139

CDD-1349	Epigenetic Reader Domain	Endocrinology
CDD-1349 (Compound 15) is a *BRDT-BD2/BRD4-BD2* selective inhibitor. CDD-1349is an analog with sixfold selectivity for BRDT-BD2 versus BRD4-BD2. CDD-1349 has an IC₅₀ of 22 nM against BRDT. CDD-1349 can be studied in research on nonhormonal contraceptive agent .

HY-177140

CDD-1147	Epigenetic Reader Domain	Others
CDD-1147 is a *BRDT-BD2* inhibitor with an IC₅₀ of 94 nM. CDD-1147 can be used in the research of non-hormonal contraceptives for men .

HY-177141

CDD-1154	Epigenetic Reader Domain	Endocrinology
CDD-1154 is an aminopyrimidine analog. CDD-1154 is a *BRDT-BD2* inhibitor (IC₅₀: 139 nM). CDD-1154 is used in male contraceptive research .

HY-150684

GXH-II-052	Epigenetic Reader Domain	Cancer
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with K_d values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .

HY-150683

NC-III-49-1	Epigenetic Reader Domain	Cancer
NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with K_d values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .

CDD-1349	other families Phenols Polyphenols Plants Pteris multifida Poir. Source Classification	Epigenetic Reader Domain
CDD-1349 (Compound 15) is a *BRDT-BD2/BRD4-BD2* selective inhibitor. CDD-1349is an analog with sixfold selectivity for BRDT-BD2 versus BRD4-BD2. CDD-1349 has an IC₅₀ of 22 nM against BRDT. CDD-1349 can be studied in research on nonhormonal contraceptive agent .

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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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BRDT-IN-2

Inhibitors & Agonists

NaturalProducts

Natural
Products