Novel inhibitors

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Cat. No.	Product Name	Field of Application
DC12641	BR101549	BR101549 (BR-101549) is a novel PPARγ non-TZD agonist with EC50 of 1.73 uM (Amax 120%)..
DC23555	BR103	BR103 is a potent, metabolically stable and highly selective small molecule agonist of complement C3a receptor (C3aR) with EC50 of 22 ± 8 nM.
DC23547	BR111	BR111 is a potent, highly selective and orally active antagonist of complement C3a receptor (C3aR) with IC50 of 85 ± 40 nM (inhibition of hC3a induced Ca2+ release on human macrophages).
DC20092	BR351	BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively. Potential tools for the molecular imaging of activated MMPs with PET.
DC20096	BR351 precursor	BR351 precursor is a precursor of BR351. BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively. Potential tools for the molecular imaging of activated MMPs with PET.
DC20827	BRACO-19	BRACO-19 is a potent small molecule Telomerase inhibitor (IC50=115 nM) that inhibits expression of human telomerase reverse transcriptase (hTERT).
DC7809	BRACO19 trihydrochloride Featured	BRACO19 is a telomerase inhibitor that stabilizes G-quadruplexes, targeting telomeric G-quadruplexes, inducing DNA damage and cell-cycle arrest.
DC20323	Bractoppin Featured	Bractoppin is a potent, small-molecule chemical inhibitor that specific selectively blocks phosphopeptide recognition by the BRCA1 tBRCT domain with binding IC50 of 74 nM; shows no inhibition for recognition of cognate biotinylated phosphopeptides to the TOPBP1 tBRCT 7/8, or GRB2 SH2 proteins; engages BRCA1 tBRCT residues recognizing pSer in the consensus motif, pSer-Pro-Thr-Phe, plus an abutting hydrophobic pocket; inhibits substrate recognition detected by Förster resonance energy transfer, and diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51; selectively interrupts BRCA1 tBRCT-dependent signals evoked by DNA damage.
DC10338	Bradykinin	Bradykinin is an active peptide that is generated by the kallikrein-kinin system. It is a inflammatory mediator and also recognized as a neuromediator and regulator of several vascular and renal functions.
DC23752	Bragsin1(Bragsin 1)	Bragsin1 (Bragsin 1) is a specific inhibitor of the ArfGEF BRAG2, affects the trans-Golgi network in a BRAG2- and Arf-dependent manner in cells (IC50=3 uM).
DC23796	BRD 0476	BRD 0476 (ML187) is a selective, moderate inhibitor of ubiquitin-specific peptidase 9X (USP9X), inhibits pancreatic β-cell apoptosis that inhibits IFN-γ-induced JAK2 and STAT1 signaling to promote β-cell survival.
DC12221	BRD 4354 Featured	BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
DC20842	BRD 7389 Featured	BRD 7389 is an inhibitor of ribosomal S6 kinases (RSK) with IC50 of 1.5 uM, 2.4 uM, and 1.2 uM for RSK1, RSK2, and RSK3, respectively.
DC20843	BRD 8184	BRD 8184 is a potent, selective HDAC6 inhibitor with IC50 of 8 nM, weakly inhibits HDAC2 and HDAC8 (IC50=0.34 and 1.33 uM),has no activity for HDAC4 (IC50>30 uM)..
DC20844	BRD 8430	BRD 8430 is a potent, selective class I HDAC inhibitor (HDAC1>2 >3) with IC50 of 69 nM/560/1300 nM for HDAC1/2/3, respectively.
DC20845	BRD 8899	BRD 8899 is a potent and selective inhibitor of the serine/threonine kinase STK33 with IC50 of 0.11 nM (25 uM ATP).
DC23341	BRD 9876	BRD 9876 is an ATP- and ADP-competitive Eg5 (kinesin-5) inhibitor with Ki of 4 nM, selectively inhibits microtubule-bound Eg5 and inhibits multiple myeloma cell growth (IC50=2.2 uM).
DC20828	BRD0209	BRD0209 is a highly selective, potent, reversible, ATP-competitive GSK3 inhibitor with IC50 of 19 nM/5 nM for GSK3α/GSK3β respectively.
DC20838	BRD0705 Featured	BRD0705 is a potent, paralog-selective GSK3α inhibitor with IC50 of 66 nM, 8-fold selectivity over GSK3β (IC50=515 nM).
DC23008	BRD10330	BRD10330 (BRD-10330) is a small molecule that upregulates IL-10 production in BMDCs.
DC20829	BRD1172	BRD1172 is a highly selective, potent, reversible, ATP-competitive GSK3 inhibitor with IC50 of 3 nM/10 nM for GSK3α/GSK3β, respectively..
DC23561	BRD1240	BRD1240 is a small-molecule probe that can suppress V-ATPase function, inhibits lysosomal acidification and blocks the maturation of autophagosomes to autolysosomes.
DC20830	BRD1652	BRD1652 is a highly selective, potent, reversible, ATP-competitive GSK3 inhibitor with IC50 of 0.4 nM/4 nM for GSK3α/GSK3β respectively.
DC10966	BRD1991	BRD1991 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity..
DC20831	BRD2492 Featured	BRD2492 is a highly potent, selective HDAC1/2 inhibitor (IC50=2/19 nM, respectively) that displays excellent selectivity versus HDAC3 (IC50=2.08 uM, ≥110-fold selectivity) and all other HDAC isoforms, increases caspase-3 activation..
DC22038	BRD2879	BRD2879 (BRD-2879) is a potent, selective inhibitor of IDH1-R132H mutant with IC50 of 50 nM, inhibits cell-based production of R-2HG with EC50 of 0.3 uM.
DC20832	BRD3308 Featured	BRD3308 is a potent, selective HDAC3 inhibitor with IC50 of 54 nM, displays >20-fold selectivity over HDAC1 and HDAC2, >500-fold selectivity over other HDAC isoforms.
DC20839	BRD3731	BRD3731 is a potent, selective GSK3β inhibitor with IC50 of 15 nM, 14-fold selectivity for GSK3β over GSK3α (IC50=215 nM).
DC10997	BRD4 degrader AT1	BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
DC12426	BRD4 inhibitor Compound V	BRD4 inhibitor Compound V is a domain-selective inhibitor of BRD4 with IC50 of 1.8 uM for BRD4 BD1, displays 6- and 16-fold selectivity for BRD4 over BRD2 and BRD3, respectively.

Novel inhibitors

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