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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
10 Results for "
BRDT-BD1
" in MedChemExpress (MCE) Product Catalog:
Products (10)
10 Results for "BRDT-BD1" in MCE Product Catalog:
2
Target:
Research Areas:
GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models [1].
Cat. No.: HY-160558
CAS No.: 2251709-91-6
Research Areas:
PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC50s of 0.059, 0.127 and 0.245 μM, respectively [1].
Cat. No.: HY-136570A
CAS No.: 2863657-79-6
Synonyms: iBET-BD1 hydrochloride
Target:
Research Areas:
GSK778 (iBET-BD1) hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively [1].
Cat. No.: HY-168628
CAS No.: 3054869-29-0
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BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC50 values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity [1].
Cat. No.: HY-183248
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Research Areas:
BRDT-IN-2 is a BRDT-BD1-preferring inhibitor (Ki=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 [1].
Cat. No.: HY-183247
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BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC50 19 nM, Ki 8.8 nM, Ka 1.6 nM, and BRDT-T IC50 56 nM, Ka 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma [1].
Cat. No.: HY-149519
CAS No.: 2468960-80-5
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Research Areas:
BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity [1].
Cat. No.: HY-153573
Synonyms: dCym-JQ1
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Research Areas:
SRG-II-19F (dCym-JQ1) is a BRDTBD1 PROTAC degrader. Its dCym moiety at one end binds to the N-terminal domain of ClpC1 (ClpC1NTD), while its JQ1 moiety at the other end binds to bromodomain 1 of BRDT (BRDTBD1). This molecule induces the degradation of BRDTBD1 by recruiting the BRDTBD1 substrate to the ClpC1P1P2 protease complex. SRG-II-19F serves as a research tool for studies related to mycobacterial protein degradation [1].
Cat. No.: HY-153574
Synonyms: pArg-JQ1
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BI01826025 (pArg-JQ1) is a BacPROTAC-type bifunctional degrader that induces the degradation of BRDTBD1-containing substrates by recruiting the ClpC1P1P2 protease system. BI01826025 binds to the BRDTBD1 substrate via its JQ1 moiety and to ClpC1 via its pArg moiety; it delivers the substrate to ClpC1, where the substrate undergoes ClpC1-mediated unfolding followed by proteolysis by ClpP1P2. BI01826025 can be used to study ClpC1P1P2-mediated targeted protein degradation and ClpC2-regulated bacterial protein homeostasis [1].
Cat. No.: HY-172210
CAS No.: 3017180-18-3
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Research Areas:
DDO-8958 is an orally active and selective BET BD1 inhibitor with a KD of 5.6 nM for BRD4 BD1. DDO-8958 exhibits low nanomolar inhibitory activity against all BET BD1 bromodomains except for BRDT BD1. DDO-8958 can inhibit the proliferation and migration, induce apoptosis and cell cycle arrest of tumor cells. DDO-8958 has anti-tumor activity [1].
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
