1949840-87-2
1949840-87-2
Chemical Structure
BCL-XL-IN-3
- CAS No.: 1949840-87-2
- Formula:C46H55N7O6S
- Molecular Weight:834.04
InChIKey: JDRWPKNPESVAQP-UOKWIRAPSA-N
SMILES: O[C@H](CO)CCNCCO[C@](C1)(C2)C[C@@](C[C@@]2(C3)C)(C[C@]13C)CN4C(C)=C(C(C=CC(N(CCC5=CC=C6)CC5=C6C(NC7=NC8=CC=CC=C8S7)=O)=N9)=C9C(O)=O)C=N4
Biological Activity: BCL-XL-IN-3 is a cell-impermeable BCL-XL inhibitor with a Ki of 16 pM. BCL-XL-IN-3 disrupts the critical hydrogen bond network via methylation of the nitrogen atom on the P2-binding amide bond, resulting in complete loss of cellular activity against BCL-XL. BCL-XL-IN-3 can be used in non-small cell lung cancer and cancer-related research[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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BCL-XL-IN-3 | BCL-XL-IN-3 is a cell-impermeable BCL-XL inhibitor with a Ki of 16 pM. BCL-XL-IN-3 disrupts the critical hydrogen bond network via methylation of the nitrogen atom on the P2-binding amide bond, resulting in complete loss of cellular activity against BCL-XL. BCL-XL-IN-3 can be used in non-small cell lung cancer and cancer-related research. | |||||||||||||||||||||
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Bcl-xL antagonist 2 | 98.86% | Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL). | ||||||||||||||||||||
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BCL-XL-IN-4 | BCL-XL-IN-4 (compound 10) is a potent and selective BCL-XL inhibitor with Ki values of 0.042, 170 nM for BCL-XL, BCL-2, respectively. BCL-XL-IN-4 shows cytotoxicity. | |||||||||||||||||||||
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BCL-xL ligand 6 | 99.06% | BCL-xL ligand 6 is a ligand for Bcl-xL that can be used in the synthesis of PROTACs. | ||||||||||||||||||||
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PROTAC Bcl-xL degrader-2 | 98.23% | PROTAC Bcl-xL degrader-2 is a selective Bcl-xL PROTAC degrader with a DC50 of 4.8 nM against Bcl-xL. PROTAC Bcl-xL degrader-2 forms a ternary complex with VHL E3 ligase, thereby redirecting the ubiquitin-proteasome system to mediate the degradation of Bcl-xL. PROTAC Bcl-xL degrader-2 triggers Apoptosis. PROTAC Bcl-xL degrader-2 can be used in the research of solid tumors and hematologic malignancies. | ||||||||||||||||||||
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Nrf2 degrader 1 | 98.77% | Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with a DC50 of 0.1-1 μM in huH1 cells. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively. Nrf2 degrader 1 can be used for the study of liver cancer, non-small cell lung cancer (NSCLC) and squamous cell carcinoma of lung cancer. | ||||||||||||||||||||
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A-1248767 | A-1248767 is a MCL-1 inhibitor (IC50=23.9 nM; Ki=0.41 nM) with anticancer activity. A-1248767, a derivative of A-1210477 (HY-12468), binds to MCL-1 with high affinity, induces the increase of intracellular MCL-1 protein, and promotes tumor cell apoptosis. | |||||||||||||||||||||
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BCL-XL-IN-5 | BCL-XL-IN-5 is an orally active, highly selective BH3-mimetic BCL-XL inhibitor with a cKi of 7.96 pM. BCL-XL-IN-5 triggers caspase-3 activation and robust PARP cleavage to initiate apoptosis in BCL-XL-dependent MOLT-4 T-cell acute lymphoblastic leukemia cells. BCL-XL-IN-5 serves as a potent selective probe for investigating BCL-XL-dependent malignancies, such as acute lymphoblastic leukemia. | |||||||||||||||||||||
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BCL-xL ligand 5 | BCL-xL ligand 5 is a Bcl-xL ligand with an IC50 of 0.5 nM. BCL-xL ligand 5 can be used for the synthesis of PROTACs, such as PROTAC Bcl-xL degrader-2 (HY-139309). | |||||||||||||||||||||
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A-1155463 | 98.02% | A-1155463, a chemical probe, is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell. A-1155463 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | ||||||||||||||||||||
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A-1331852 | 99.93% | A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM. | ||||||||||||||||||||
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References
- [1]. Judd AS, et al. BCL-X-targeting antibody-drug conjugates are active in preclinical models and mitigate on-mechanism toxicity of small-molecule inhibitors. Science advances. 2024 Oct 04;10(40):eado7120. [Content Brief]
- [2]. Tao ZF, et al. Bcl-xl inhibitory compounds having low cell permeability and antibody drug conjugates including the same. WO2016094509 A1. 2016 Jun 16.
