Recombinant:Article Title: Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.
Article Snippet: REAGENT or RESOURCE SOURCE IDENTIFIER Experimental Models: Cell Lines ZR751 ATCC Cat#CRL-1500 CAMA1 ATCC Cat#HTB-21 HCC1599 ATCC Cat#CRL-2331 SNU1528 KLCB Cat#01528 T47D ATCC Cat#HTB-133 HCC1500 ATCC Cat#CRL-2329 T47DKBLUC ATCC Cat#CRL-286 YMB1 JCRB Cat#JCRB0823 HCC1187 ATCC Cat#CRL-2322 IOWA1T ATCC Cat#CRL-3292 HCC1419 ATCC Cat#CRL-2326 HCC2157 ATCC Cat#CRL-2340 HCC1428 ATCC Cat#CRL-2327 CCD1068SK ATCC Cat#CRL-2086 CCD1069SK ATCC Cat#CRL-2089 HS578T ATCC Cat#HTB-126 CCD1097SK ATCC Cat#CRL-2124 CCD1065SK ATCC Cat#CRL-2077 CCD1095SK ATCC Cat#CRL-2122 MDAMB453 CASTCC Cat#TCHu233 OCUBM RCB Cat#RCB0881 HCC1569 ATCC Cat#CRL-2330 HS739T ATCC Cat#CRL-7477 HCC2218 ATCC Cat#CRL-2343 MDAMB157 ATCC Cat#HTB-24 MX1 NCI Cat#MX1 JIMT1 DSMZ Cat#ACC-589 AU565 ATCC Cat#CRL-2351 HCC1937 ATCC Cat#CRL-2336 MCF7 ATCC Cat#HTB-22 MDAMB231 ATCC Cat#HTB-26 MDAMB361 ATCC Cat#HTB-27 SKBR3 ATCC Cat#HTB-30 HBL100 CASTCC Cat#GNHu10 HCC1806 ATCC Cat#CRL-2335 HCC70 ATCC Cat#CRL-2315 DU4475 ATCC Cat#HTB-123 HCC1954 ATCC Cat#CRL-2338 BT549 ATCC Cat#HTB-122 BT20 ATCC Cat#HTB-19 MDAMB468 ATCC Cat#HTB-132 MDAMB436 ATCC Cat#HTB-130 SNU1958 KLCB Cat#01958 ZR7530 ATCC Cat#CRL-1504 (Continued on next page) Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 e1 .. REAGENT or RESOURCE SOURCE IDENTIFIER BT474 ATCC Cat#HTB-20 MRKNU1 HSRRB/JCRB Cat#JCRB0628 MDAMB415 ATCC Cat#HTB-128 BT20NKR SNU/KCLB Cat60071 UACC3133 ATCC Cat#CRL-2988 HCC1143 ATCC Cat#CRL-2321 MDAMB175VII ATCC Cat#HTB-25 UACC2087 ATCC Cat#CRL-3180 UACC893 ATCC Cat#CRL-1902 OCUBF RCB Cat#RCB0882 EVSAT DSMZ Cat#CVCL_1207 CAL51 DSMZ Cat#ACC-302 MFM223 DSMZ Cat#ACC-422 EFM19 DSMZ Cat#ACC-231 CAL120 DSMZ Cat#ACC-459 EFM192A DSMZ Cat#ACC-258 PDX-23T (Vaillant et al., 2013)60 N/A PDX-50T (Vaillant et al., 2013)60 N/A PDX-1105T (Whittle et al., 2020)62 N/A ST340 Xenostart N/A Experimental Models: Organisms/Strains NSG mice The Jackson Laboratory Cat#5557 Foxn1nu nude mice The Jackson Laboratory Cat#007850 Chemicals, peptides, and recombinant proteins RPMI1640 Gibco Cat#11875-093 RPMI1640 Life Technologies Cat#11875085 DMEM Invitrogen Cat#11965118 EMEM ATCC Cat#30-2003 FBS Gibco Cat#10082147 Fetal Bovine Serum (FBS) Life Technologies Cat#26140079 Glutamine Invitrogen Cat#35050079 Sodium Pyruvate Invitrogen Cat#11360070 NEAA Invitrogen Cat#11140076 293T Lenti-X cells Clontech Cat#632180 Lentiviral Packaging Mix Sigma Cat#SHP-001 Lipofectamine 2000 ThermoFisher Cat#11668019 Polystyrene flat bottom cell culture microplate Thermo Fisher Scientific Cat#07-000-162 Hydrochloric acid Thermo Fisher Scientific Cat#SA56-1 Blocking buffer Thermo Fisher Scientific Cat#37542 Luminescent GLO substrate R&D System Cat#DY993 Poly-D-Lysine coated black 96-well microplates Corning Cat#3842 Clear U-bottom, polypropylene plates Corning Cat#3365 Triton X-100/PBS Thermo Fisher Scientific Cat#NC0478124 PMSF Sigma Cat#252549 Blocking buffer Thermo Fisher Scientific Cat#37535 (Continued on next page) e2 Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 .. REAGENT or RESOURCE SOURCE IDENTIFIER Corning Matrigel Basement Membrane Matrix Corning Cat#354234 FastPrep Lysing Matrix A Tubes Millipore Cat#116910100 phenylmethylsulfonyl fluoride Sigma Aldrich Cat#18830-5G Proteinase Inhibitor Sigma Aldrich Cat#1187358001 Sodium Butyrate Millipore Sigma Cat#TR1008G Coomassie Plus Better Bradford Assay Pierce Cat#23238 Pre-Diluted BSA Standards Thermo Fisher, Cat#23208 96-well MSD Plates Meso Scale Discovery Cat#L15XA-3/L11XA-3 PBS (Phosphate Buffered Saline) GIBCO Cat#10010 KPL Wash Buffer Sera Care Cat#5150-0008 SuperBlock Solution Thermo Fisher Cat#037535 Reagent Diluent Concentrate 2 R&D Systems Cat#DY995 StartingBlock TBS Buffer Thermo Fisher Cat#037542 Read Buffer T Meso Scale Discovery Cat#R92TD-1 Recombinant H3K23Ac Protein Active Motif Cat#31255 Complete Protease Inhibitor Cocktail (50x) MilliporeSigma Cat#11697498001 PhosSTOP MilliporeSigma Cat#4906837001 500 nM Sodium Butyrate MilliporeSigma Cat#TR1008G Pre-Diluted BSA Standards ThermoFisher Cat#23208 Coomassie Plus Better Bradford Assay Reagent Pierce Cat#23238 NuPAGE LDS Sample Buffer (4x) ThermoFisher Cat#NP0007 NuPAGE Sample Reducing Agent (10x) ThermoFisher Cat#NP0009 4-12% Gradient 26 well Biorad Criterion XT Biorad Cat#3450125 XT MES Running Buffer Biorad Cat#1610789 Odyssey Protein Molecular Weight Ladder LI-COR Cat#92840000 Transblot Turbo Midi .2um PVDF Membrane Biorad Cat#1704157 Trans-Blot Turbo Transfer System Biorad Cat#1704150 Odyssey Blocking Buffer LI-COR Cat#92740000 protease inhibitors Roche Cat#11697498001 RNase Thermo Scientific Cat#FEREN0531 proteinase K Invitrogen Cat#25530049 Ampure XP beads Beckman Coulter Cat#A63880 Dynabeads Protein G Invitrogen Cat#10004D Trizol reagent Invitrogen Cat#15596-018 D1000 Screen Tape Agilent Technologies Cat#5067-5584 Critical commercial assays Histone Purification Mini Kit Active Motif Cat#40026 iScript reverse transcription kit Bio-Rad Cat#1708891 mRNA Catcher plus kit ThermoFisher Cat#K157003 EpiQuik Total Histone Extraction Kit EpiGentek Cat#OP-0006-100 (Continued on next page) Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 e3
Cell Culture:Article Title: Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.
Article Snippet: REAGENT or RESOURCE SOURCE IDENTIFIER Experimental Models: Cell Lines ZR751 ATCC Cat#CRL-1500 CAMA1 ATCC Cat#HTB-21 HCC1599 ATCC Cat#CRL-2331 SNU1528 KLCB Cat#01528 T47D ATCC Cat#HTB-133 HCC1500 ATCC Cat#CRL-2329 T47DKBLUC ATCC Cat#CRL-286 YMB1 JCRB Cat#JCRB0823 HCC1187 ATCC Cat#CRL-2322 IOWA1T ATCC Cat#CRL-3292 HCC1419 ATCC Cat#CRL-2326 HCC2157 ATCC Cat#CRL-2340 HCC1428 ATCC Cat#CRL-2327 CCD1068SK ATCC Cat#CRL-2086 CCD1069SK ATCC Cat#CRL-2089 HS578T ATCC Cat#HTB-126 CCD1097SK ATCC Cat#CRL-2124 CCD1065SK ATCC Cat#CRL-2077 CCD1095SK ATCC Cat#CRL-2122 MDAMB453 CASTCC Cat#TCHu233 OCUBM RCB Cat#RCB0881 HCC1569 ATCC Cat#CRL-2330 HS739T ATCC Cat#CRL-7477 HCC2218 ATCC Cat#CRL-2343 MDAMB157 ATCC Cat#HTB-24 MX1 NCI Cat#MX1 JIMT1 DSMZ Cat#ACC-589 AU565 ATCC Cat#CRL-2351 HCC1937 ATCC Cat#CRL-2336 MCF7 ATCC Cat#HTB-22 MDAMB231 ATCC Cat#HTB-26 MDAMB361 ATCC Cat#HTB-27 SKBR3 ATCC Cat#HTB-30 HBL100 CASTCC Cat#GNHu10 HCC1806 ATCC Cat#CRL-2335 HCC70 ATCC Cat#CRL-2315 DU4475 ATCC Cat#HTB-123 HCC1954 ATCC Cat#CRL-2338 BT549 ATCC Cat#HTB-122 BT20 ATCC Cat#HTB-19 MDAMB468 ATCC Cat#HTB-132 MDAMB436 ATCC Cat#HTB-130 SNU1958 KLCB Cat#01958 ZR7530 ATCC Cat#CRL-1504 (Continued on next page) Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 e1 .. REAGENT or RESOURCE SOURCE IDENTIFIER BT474 ATCC Cat#HTB-20 MRKNU1 HSRRB/JCRB Cat#JCRB0628 MDAMB415 ATCC Cat#HTB-128 BT20NKR SNU/KCLB Cat60071 UACC3133 ATCC Cat#CRL-2988 HCC1143 ATCC Cat#CRL-2321 MDAMB175VII ATCC Cat#HTB-25 UACC2087 ATCC Cat#CRL-3180 UACC893 ATCC Cat#CRL-1902 OCUBF RCB Cat#RCB0882 EVSAT DSMZ Cat#CVCL_1207 CAL51 DSMZ Cat#ACC-302 MFM223 DSMZ Cat#ACC-422 EFM19 DSMZ Cat#ACC-231 CAL120 DSMZ Cat#ACC-459 EFM192A DSMZ Cat#ACC-258 PDX-23T (Vaillant et al., 2013)60 N/A PDX-50T (Vaillant et al., 2013)60 N/A PDX-1105T (Whittle et al., 2020)62 N/A ST340 Xenostart N/A Experimental Models: Organisms/Strains NSG mice The Jackson Laboratory Cat#5557 Foxn1nu nude mice The Jackson Laboratory Cat#007850 Chemicals, peptides, and recombinant proteins RPMI1640 Gibco Cat#11875-093 RPMI1640 Life Technologies Cat#11875085 DMEM Invitrogen Cat#11965118 EMEM ATCC Cat#30-2003 FBS Gibco Cat#10082147 Fetal Bovine Serum (FBS) Life Technologies Cat#26140079 Glutamine Invitrogen Cat#35050079 Sodium Pyruvate Invitrogen Cat#11360070 NEAA Invitrogen Cat#11140076 293T Lenti-X cells Clontech Cat#632180 Lentiviral Packaging Mix Sigma Cat#SHP-001 Lipofectamine 2000 ThermoFisher Cat#11668019 Polystyrene flat bottom cell culture microplate Thermo Fisher Scientific Cat#07-000-162 Hydrochloric acid Thermo Fisher Scientific Cat#SA56-1 Blocking buffer Thermo Fisher Scientific Cat#37542 Luminescent GLO substrate R&D System Cat#DY993 Poly-D-Lysine coated black 96-well microplates Corning Cat#3842 Clear U-bottom, polypropylene plates Corning Cat#3365 Triton X-100/PBS Thermo Fisher Scientific Cat#NC0478124 PMSF Sigma Cat#252549 Blocking buffer Thermo Fisher Scientific Cat#37535 (Continued on next page) e2 Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 .. REAGENT or RESOURCE SOURCE IDENTIFIER Corning Matrigel Basement Membrane Matrix Corning Cat#354234 FastPrep Lysing Matrix A Tubes Millipore Cat#116910100 phenylmethylsulfonyl fluoride Sigma Aldrich Cat#18830-5G Proteinase Inhibitor Sigma Aldrich Cat#1187358001 Sodium Butyrate Millipore Sigma Cat#TR1008G Coomassie Plus Better Bradford Assay Pierce Cat#23238 Pre-Diluted BSA Standards Thermo Fisher, Cat#23208 96-well MSD Plates Meso Scale Discovery Cat#L15XA-3/L11XA-3 PBS (Phosphate Buffered Saline) GIBCO Cat#10010 KPL Wash Buffer Sera Care Cat#5150-0008 SuperBlock Solution Thermo Fisher Cat#037535 Reagent Diluent Concentrate 2 R&D Systems Cat#DY995 StartingBlock TBS Buffer Thermo Fisher Cat#037542 Read Buffer T Meso Scale Discovery Cat#R92TD-1 Recombinant H3K23Ac Protein Active Motif Cat#31255 Complete Protease Inhibitor Cocktail (50x) MilliporeSigma Cat#11697498001 PhosSTOP MilliporeSigma Cat#4906837001 500 nM Sodium Butyrate MilliporeSigma Cat#TR1008G Pre-Diluted BSA Standards ThermoFisher Cat#23208 Coomassie Plus Better Bradford Assay Reagent Pierce Cat#23238 NuPAGE LDS Sample Buffer (4x) ThermoFisher Cat#NP0007 NuPAGE Sample Reducing Agent (10x) ThermoFisher Cat#NP0009 4-12% Gradient 26 well Biorad Criterion XT Biorad Cat#3450125 XT MES Running Buffer Biorad Cat#1610789 Odyssey Protein Molecular Weight Ladder LI-COR Cat#92840000 Transblot Turbo Midi .2um PVDF Membrane Biorad Cat#1704157 Trans-Blot Turbo Transfer System Biorad Cat#1704150 Odyssey Blocking Buffer LI-COR Cat#92740000 protease inhibitors Roche Cat#11697498001 RNase Thermo Scientific Cat#FEREN0531 proteinase K Invitrogen Cat#25530049 Ampure XP beads Beckman Coulter Cat#A63880 Dynabeads Protein G Invitrogen Cat#10004D Trizol reagent Invitrogen Cat#15596-018 D1000 Screen Tape Agilent Technologies Cat#5067-5584 Critical commercial assays Histone Purification Mini Kit Active Motif Cat#40026 iScript reverse transcription kit Bio-Rad Cat#1708891 mRNA Catcher plus kit ThermoFisher Cat#K157003 EpiQuik Total Histone Extraction Kit EpiGentek Cat#OP-0006-100 (Continued on next page) Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 e3
Blocking Assay:Article Title: Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.
Article Snippet: REAGENT or RESOURCE SOURCE IDENTIFIER Experimental Models: Cell Lines ZR751 ATCC Cat#CRL-1500 CAMA1 ATCC Cat#HTB-21 HCC1599 ATCC Cat#CRL-2331 SNU1528 KLCB Cat#01528 T47D ATCC Cat#HTB-133 HCC1500 ATCC Cat#CRL-2329 T47DKBLUC ATCC Cat#CRL-286 YMB1 JCRB Cat#JCRB0823 HCC1187 ATCC Cat#CRL-2322 IOWA1T ATCC Cat#CRL-3292 HCC1419 ATCC Cat#CRL-2326 HCC2157 ATCC Cat#CRL-2340 HCC1428 ATCC Cat#CRL-2327 CCD1068SK ATCC Cat#CRL-2086 CCD1069SK ATCC Cat#CRL-2089 HS578T ATCC Cat#HTB-126 CCD1097SK ATCC Cat#CRL-2124 CCD1065SK ATCC Cat#CRL-2077 CCD1095SK ATCC Cat#CRL-2122 MDAMB453 CASTCC Cat#TCHu233 OCUBM RCB Cat#RCB0881 HCC1569 ATCC Cat#CRL-2330 HS739T ATCC Cat#CRL-7477 HCC2218 ATCC Cat#CRL-2343 MDAMB157 ATCC Cat#HTB-24 MX1 NCI Cat#MX1 JIMT1 DSMZ Cat#ACC-589 AU565 ATCC Cat#CRL-2351 HCC1937 ATCC Cat#CRL-2336 MCF7 ATCC Cat#HTB-22 MDAMB231 ATCC Cat#HTB-26 MDAMB361 ATCC Cat#HTB-27 SKBR3 ATCC Cat#HTB-30 HBL100 CASTCC Cat#GNHu10 HCC1806 ATCC Cat#CRL-2335 HCC70 ATCC Cat#CRL-2315 DU4475 ATCC Cat#HTB-123 HCC1954 ATCC Cat#CRL-2338 BT549 ATCC Cat#HTB-122 BT20 ATCC Cat#HTB-19 MDAMB468 ATCC Cat#HTB-132 MDAMB436 ATCC Cat#HTB-130 SNU1958 KLCB Cat#01958 ZR7530 ATCC Cat#CRL-1504 (Continued on next page) Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 e1 .. REAGENT or RESOURCE SOURCE IDENTIFIER BT474 ATCC Cat#HTB-20 MRKNU1 HSRRB/JCRB Cat#JCRB0628 MDAMB415 ATCC Cat#HTB-128 BT20NKR SNU/KCLB Cat60071 UACC3133 ATCC Cat#CRL-2988 HCC1143 ATCC Cat#CRL-2321 MDAMB175VII ATCC Cat#HTB-25 UACC2087 ATCC Cat#CRL-3180 UACC893 ATCC Cat#CRL-1902 OCUBF RCB Cat#RCB0882 EVSAT DSMZ Cat#CVCL_1207 CAL51 DSMZ Cat#ACC-302 MFM223 DSMZ Cat#ACC-422 EFM19 DSMZ Cat#ACC-231 CAL120 DSMZ Cat#ACC-459 EFM192A DSMZ Cat#ACC-258 PDX-23T (Vaillant et al., 2013)60 N/A PDX-50T (Vaillant et al., 2013)60 N/A PDX-1105T (Whittle et al., 2020)62 N/A ST340 Xenostart N/A Experimental Models: Organisms/Strains NSG mice The Jackson Laboratory Cat#5557 Foxn1nu nude mice The Jackson Laboratory Cat#007850 Chemicals, peptides, and recombinant proteins RPMI1640 Gibco Cat#11875-093 RPMI1640 Life Technologies Cat#11875085 DMEM Invitrogen Cat#11965118 EMEM ATCC Cat#30-2003 FBS Gibco Cat#10082147 Fetal Bovine Serum (FBS) Life Technologies Cat#26140079 Glutamine Invitrogen Cat#35050079 Sodium Pyruvate Invitrogen Cat#11360070 NEAA Invitrogen Cat#11140076 293T Lenti-X cells Clontech Cat#632180 Lentiviral Packaging Mix Sigma Cat#SHP-001 Lipofectamine 2000 ThermoFisher Cat#11668019 Polystyrene flat bottom cell culture microplate Thermo Fisher Scientific Cat#07-000-162 Hydrochloric acid Thermo Fisher Scientific Cat#SA56-1 Blocking buffer Thermo Fisher Scientific Cat#37542 Luminescent GLO substrate R&D System Cat#DY993 Poly-D-Lysine coated black 96-well microplates Corning Cat#3842 Clear U-bottom, polypropylene plates Corning Cat#3365 Triton X-100/PBS Thermo Fisher Scientific Cat#NC0478124 PMSF Sigma Cat#252549 Blocking buffer Thermo Fisher Scientific Cat#37535 (Continued on next page) e2 Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 .. REAGENT or RESOURCE SOURCE IDENTIFIER Corning Matrigel Basement Membrane Matrix Corning Cat#354234 FastPrep Lysing Matrix A Tubes Millipore Cat#116910100 phenylmethylsulfonyl fluoride Sigma Aldrich Cat#18830-5G Proteinase Inhibitor Sigma Aldrich Cat#1187358001 Sodium Butyrate Millipore Sigma Cat#TR1008G Coomassie Plus Better Bradford Assay Pierce Cat#23238 Pre-Diluted BSA Standards Thermo Fisher, Cat#23208 96-well MSD Plates Meso Scale Discovery Cat#L15XA-3/L11XA-3 PBS (Phosphate Buffered Saline) GIBCO Cat#10010 KPL Wash Buffer Sera Care Cat#5150-0008 SuperBlock Solution Thermo Fisher Cat#037535 Reagent Diluent Concentrate 2 R&D Systems Cat#DY995 StartingBlock TBS Buffer Thermo Fisher Cat#037542 Read Buffer T Meso Scale Discovery Cat#R92TD-1 Recombinant H3K23Ac Protein Active Motif Cat#31255 Complete Protease Inhibitor Cocktail (50x) MilliporeSigma Cat#11697498001 PhosSTOP MilliporeSigma Cat#4906837001 500 nM Sodium Butyrate MilliporeSigma Cat#TR1008G Pre-Diluted BSA Standards ThermoFisher Cat#23208 Coomassie Plus Better Bradford Assay Reagent Pierce Cat#23238 NuPAGE LDS Sample Buffer (4x) ThermoFisher Cat#NP0007 NuPAGE Sample Reducing Agent (10x) ThermoFisher Cat#NP0009 4-12% Gradient 26 well Biorad Criterion XT Biorad Cat#3450125 XT MES Running Buffer Biorad Cat#1610789 Odyssey Protein Molecular Weight Ladder LI-COR Cat#92840000 Transblot Turbo Midi .2um PVDF Membrane Biorad Cat#1704157 Trans-Blot Turbo Transfer System Biorad Cat#1704150 Odyssey Blocking Buffer LI-COR Cat#92740000 protease inhibitors Roche Cat#11697498001 RNase Thermo Scientific Cat#FEREN0531 proteinase K Invitrogen Cat#25530049 Ampure XP beads Beckman Coulter Cat#A63880 Dynabeads Protein G Invitrogen Cat#10004D Trizol reagent Invitrogen Cat#15596-018 D1000 Screen Tape Agilent Technologies Cat#5067-5584 Critical commercial assays Histone Purification Mini Kit Active Motif Cat#40026 iScript reverse transcription kit Bio-Rad Cat#1708891 mRNA Catcher plus kit ThermoFisher Cat#K157003 EpiQuik Total Histone Extraction Kit EpiGentek Cat#OP-0006-100 (Continued on next page) Cell Chemical Biology 30, 1191–1210.e1–e20, October 19, 2023 e3
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