Click Chemistry

Tos-pentane-azide is a linker containing an azide group and a tosyl group. The azide group can react with alkyne, BCN, DBCO via Click Chemistry to yield a stable triazole linkage. The tosyl group is a good leaving group for nucleophilic substitution reactions. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

t-Boc-Aminooxy-pentane-azide is a linker containing an azide group and Boc-protected amino group. The azide group can react with alkyne, BCN, DBCO via Click Chemistry to yield a stable triazole linkage. The Boc group can be deprotected under mild acidic conditions to form the free amine. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

t-Boc-Aminooxy-pentane-amine is a linker containing an aminooxy group and a primary amine. The aminooxy group can be used in bioconjugation. It reacts with an aldehyde to form an oxime bond. If a reductant is used, it will form a hydroxylamine linkage. The amino group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

5-azidopentan-1-amine is a linker containing an amino group with an azide group. The amino group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The azide group can react with alkyne, BCN, DBCO via Click Chemistry to yield a stable triazole linkage. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

BAY-299 is a potent and selective inhibitor of BRD1 and the second bromodomain of TAF1 (Transcription initiation factor TFIID subunits. BAY-299 has IC50 values of 6-67 and 8-13 nM for BRD1 and TAF1 inhibitor, respectively. BAY-299 shows selectivity over other bromodomains (>30-fold over other members of the BRPF family; BRD9 and ATAD2; >300-fold over BRD4). Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor. BAZ2-ICR is a small molecule inhibitor of BAZ2A (Kd = 109 nM; IC50 = 130 nM) and BAZ2B (Kd = 170 nM; IC50 = 180 nM) bromodomains. BAZ2A is an essential component of the nucleolar remodeling complex (NoRC), which mediates recruitment of histone modifyine enzymes and DNA methylase involved in the silencing of ribosomal RNA transcription by RNA polymerase I. BAZ2B is believed to be involved in regulating nucleosome mobilization along linear DNA. BAZ2-ICR also exhibits 15-fold selectivity for the BAZ2 bromodomain over the CERC2 bromodomain and >100-fold selectivity over a range of other bromodomains. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

BI 9564 inhibits BRD9 and BRD7 bromodomains and exhibits no significant off-target pharmacology against a panel of 324 kinases and 55 GPCRs at concentrations less than 5 µM. BI 9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 µM and 1 µM, respectively. Inhibits proliferation of AML cell lines in vitro and reduces AML tumor xenograft growth in vivo. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

Bromosporine is a broad spectrum, non-selective bromodomain inhibitor. In HeLa cells, bromosporine accelerates FRAP recovery of BRD4 and CREBBP at 1μM. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

CPI-203 is a primary amide analog of (+)-JQ1, which has shown superior bioavailability with oral or i.p. administration. CPI-203 downregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. CPI-203 also arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.