BTSA1.2

  Cat. No.:  DC59120   Featured
Chemical Structure
2254256-66-9
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More than 5000 active chemicals with high quality for research!
Field of application
BTSA1.2 is a rationalized BTSA1 analog with improved binding to BAX, cellular cytotoxicity, and better toleratence in vivo. Combination of BTSA1.2 with Navitoclax demonstrates synergistic efficacy in apoptosis-resistant cancer cells, xenografts, and patient-derived tumors while sparing healthy tissues.
Cas No.: 2254256-66-9
Chemical Name: 3H -Pyrazol-3-one, 4-[2-(4,5-dimethyl-2-thiazolyl)diazenyl]-2,4-dihydro-5-phenyl-2-(4-phenyl-2-thiazolyl)- (ACI)
SMILES: O=C1N(N=C(C=2C=CC=CC2)C1N=NC3=NC(=C(S3)C)C)C4=NC(=CS4)C=5C=CC=CC5
Formula: C23H18N6Os2
M.Wt: 458.56
Purity: >98%
Sotrage: -20
Publication: [1] Promising approach against treatment-resistant cancer. Retrieved Mar 8th, 2022 from https://medicalxpress.com/news/2022-03-approach-treatment-resistant-cancer.html [2] Andrea Lopez et al, Co-targeting of BAX and BCL-XL proteins broadly overcomes resistance to apoptosis in cancer, Nature Communications (2022). DOI: 10.1038/s41467-022-28741-7
Description: BTSA1.2 is a rationalized BTSA1 analog with improved binding to BAX, cellular cytotoxicity, and better toleratence in vivo. Combination of BTSA1.2 with Navitoclax demonstrates synergistic efficacy in apoptosis-resistant cancer cells, xenografts, and patient-derived tumors while sparing healthy tissues.
Target: BAX
References: [1] Promising approach against treatment-resistant cancer. Retrieved Mar 8th, 2022 from https://medicalxpress.com/news/2022-03-approach-treatment-resistant-cancer.html [2] Andrea Lopez et al, Co-targeting of BAX and BCL-XL proteins broadly overcomes resistance to apoptosis in cancer, Nature Communications (2022). DOI: 10.1038/s41467-022-28741-7
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC59120 BTSA1.2 BTSA1.2 is a rationalized BTSA1 analog with improved binding to BAX, cellular cytotoxicity, and better toleratence in vivo. Combination of BTSA1.2 with Navitoclax demonstrates synergistic efficacy in apoptosis-resistant cancer cells, xenografts, and patient-derived tumors while sparing healthy tissues.
DC70246 BFL-1 inhibitor 4E14 BFL-1 inhibitor 4E14 (4E14) is a potent, selective, covalent BFL-1 inhibitor that disrupt BH3-binding activity with IC50 of 1.3 uM, targets a unique C55 residue in the BFL-1 groove.4E14 blocks BFL-1 suppression of BAX-mediated mitochondrial apoptosis.
DC50166 Bim-IN-1 Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity.
DC28441 BTSA1 BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediat
DC12064 VU0661013 VU661013 is a potent and selective MCL-1 inhibitor.
DC8444 Sabutoclax Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
DC10137 S63845 S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor; binds human MCL1 with a Kd of 0.19 nM.
DC12163 S55746 (BLC201) S55746 (BLC201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity[1].
DC7233 Pifithrin-u Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
DC7217 Obatoclax (GX15-070) Obatoclax (GX15-070) is Bcl-2 homology domain-3 (BH3) mimetic, antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L).
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