|
T38622 |
Bcl-xL antagonist 2
|
|
BCL
|
|
Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM. Bcl-xL antagonist 2 induces apoptosis in cancer cells and can be used in studies about chronic lymphocytic l... |
|
T10483 |
Lisaftoclax
|
Bcl-2/Bcl-xl inhibitor 1,APG-2575 |
BCL
|
|
Lisaftoclax (Bcl-2/Bcl-xl inhibitor 1) is an oral dual inhibitor of Bcl-2 and Bcl-xl, with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively. Lisaftoclax is used to treat chronic lymphocytic leukemia (CLL... |
|
T33467 |
MOMIPP
|
|
PI3K
|
|
MOMIPP is a PIKfyve inhibitor and a macropinocytosis inducer. MOMIPP readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts[1][2]. |
|
T18363 |
Monoethyl pimelate
|
|
Others
,
PROTAC Linker
|
|
Monoethyl pimelate is a <b >PROTAC linker, which refers to the alkyl/ether composition. Monoethyl pimelate can be used in the synthesis of (S,R,S)-AHPC-Me-C7 ester, a specific BCL-XL PROTAC degrader[1]. |
|
T80221 |
TAT-BH4 (Bcl-xL)
|
|
Apoptosis
|
|
TAT-BH4 (Bcl-xL), primarily localized at the mitochondria, inhibits apoptotic cell death. This compound comprises an N-terminal eosin-labeled cysteine and the protein transduction domain of the HIV TAT protein (amino aci... |
|
T73999 |
PROTAC Bcl-xL degrader-3
|
|
|
|
PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader. |
|
T74138 |
PROTAC Bcl-xL degrader-2
|
|
|
|
PROTAC Bcl-xL degrader-2, based on von Hippel-Lindau ligand, is a potent degrader of Bcl-xL (a Bcl-2 family member), demonstrating an IC 50 of 0.6 nM. |
|
T80222 |
TAT-BH4 (Bcl-xL) (TFA)
|
|
Apoptosis
|
|
"TAT-BH4 (Bcl-xL) TFA, primarily localized at the mitochondria, inhibits apoptotic cell death. This compound comprises an eosin-labeled cysteine at the N-terminal and the protein transduction domain from the HIV TAT prot... |
|
T74137 |
PROTAC Bcl-xL ligand-1
|
|
|
|
PROTAC Bcl-xL ligand-1 serves as a ligand targeting Bcl-xL, essential in synthesizing PROTACs [1]. |
|
T73957 |
PROTAC Bcl-xL degrader-1
|
|
|
|
PROTAC Bcl-xL degrader-1 is a potent PROTAC composed of a Bcl-xL (Bcl-2 family member) ligand-binding group, a linker, and an IAP E3 ligases binding group, demonstrating effectiveness as a Bcl-xL degrader. It exhibits to... |
|
T12412L |
PDK4-IN-1 hydrochloride
|
|
Apoptosis
,
PDK
|
|
|
|
T8656 |
CAY10404
|
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T |
Apoptosis
,
Akt
,
COX
|
|
CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSC-LC cel... |
|
T6748 |
A-1155463
|
A 1155463,A1155463 |
BCL
|
|
A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM). |
|
T14071 |
A-385358
|
|
BCL
|
|
A-385358 is a selective Bcl-xL inhibitor with Kis of 0.80 nM for Bcl-xL and 67 nM for Bcl-2, respectively. |
|
T6281 |
TW-37
|
TW 37 |
BCL
|
|
TW-37 is an nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 (Ki: 0.29/1.11/0.26 μM). |
|
T6650 |
Sabutoclax
|
BI-97C1 |
BCL
|
|
Sabutoclax (BI-97C1)(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. |
|
T2099 |
ABT-737
|
|
Mitophagy
,
BCL
,
Autophagy
|
|
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w (EC50s: 78.7/30.3/197.8 nM). |
|
T2101 |
Navitoclax
|
ABT-263 |
BCL
|
|
Navitoclax (ABT-263) is a Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM) with potent and oral activity. Navitoclax has antitumor activity and induces apoptosis. |
|
T1493 |
BH3I-1
|
BHI1 |
BCL
,
E1/E2/E3 Enzyme
|
|
BH3I-1 (BHI1) is a Bcl-2 antagonist. |
|
T6396 |
(R)-(-)-Gossypol acetic acid
|
(-)-Gossypol acetic acid,AT-101 (acetic acid),(R)-Gossypol acetic acid,AT101,AT101 acetate |
BCL
,
Autophagy
|
|
(R)-(-)-Gossypol acetic acid (AT101 acetate) , the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID. Phase 2. |
|
T2119 |
Venetoclax
|
GDC-0199,ABT 199,ABT-199,ABT199 |
BCL
,
Autophagy
|
|
Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48/245 nM). Venetoclax induces a... |
|
T1980 |
HA14-1
|
|
BCL
|
|
HA14-1, a Bcl-2/Bcl-XL antagonist, is a non-peptidic ligand of a Bcl-2 surface pocket (IC50: ~9 μM). |
|
T39910 |
Desmorpholinyl Navitoclax-NH-Me
|
Desmorpholinyl ABT-263-NH-Me,Desmorpholinyl Navitoclax-NH-Me |
BCL
|
|
Desmorpholinyl Navitoclax-NH-Me (Desmorpholinyl ABT-263-NH-Me) is a Bcl-xL inhibitor, which can be employed alongside a CRBN ligand to synthesize XZ739, a PROTAC BCL-XL degrader [1] [2]. |
|
T12186 |
Navitoclax-piperazine
|
ABT-263-piperazine |
BCL
,
Ligands for Target Protein for PROTAC
|
|
Navitoclax-piperazine (ABT-263-piperazine) is an inhibitor of B-cell lymphoma extra large (BCL-XL). |
|
T11944 |
Maritoclax
|
Marinopyrrole A |
BCL
|
|
Maritoclax (Marinopyrrole A) (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor, shows >8 fold selectivity than BCL-xl (IC50 > 80 μM),with an IC50 value of 10.1 μM. |
|
T6749 |
A-1331852
|
|
BCL
|
|
A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases. |
|
T40412L |
BAD (103-127) (human) acetate
|
BAD (103-127) (human) acetate (331762-68-6 Free base) |
Others
|
|
BAD (103-127) (human) acetate is a 25-mer Bad polypeptide from the BAD BH3 domain that antagonizes the effects of Bcl-xl. |
|
T16436 |
PBOX 6
|
PBOX-6 |
Apoptosis
|
|
PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound with anticancer and antitumor activity that inhibits breast cancer cell growth in vitro and selectively induces apoptosis in leukemia cells via c-Jun NH2 terminal kin... |
|
T9014 |
SKI-178
|
|
Apoptosis
,
S1P Receptor
|
|
SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during ... |
|
T3708 |
BP-1-102
|
|
STAT
|
|
BP-1-102 is an orally active, effective and specific STAT3 inhibitor. BP-1-102 binds Stat3 (Kd: 504 nM), then blocks Stat3-phosphotyrosine (pTyr) peptide interactions and Stat3 activation (4-6.8 μM), and selectively inhi... |
|
T9382 |
Thalidomide-NH-C2-PEG3-OH
|
H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethyl]amino]- |
E3 Ligase Ligand-Linker Conjugate
|
|
Thalidomide-NH-C2-PEG3-OH (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethyl]amino]-) is an E3 ligase ligand-linker conjugate. |
|
T13337 |
WEHI-539 hydrochloride
|
|
BCL
|
|
WEHI-539 hydrochloride is a selective Bcl-XL inhibitor (IC50: 1.1 nM). |
|
T10577 |
BM 957
|
|
BCL
|
|
BM 957 is an effective Bcl-2 and Bcl-xL inhibitor (Kis: 1.2 and <1 nM; IC50s: 5.4 and 6.0 nM). |
|
T39961 |
Bcl-2-IN-2
|
|
|
|
Bcl-2-IN-2 is a highly potent and selective inhibitor targeting Bcl-2 and Bcl-xL. It displays an IC50 value of 0.034 nM, suggesting its strong inhibitory activity specifically against Bcl-2. Additionally, Bcl-2-IN-2 exhi... |
|
T13337L |
WEHI-539
|
|
BCL
|
|
WEHI-539 is a selective Bcl-XL inhibitor (IC50: 1.1 nM). |
|
T13459 |
(+)-Apogossypol
|
Apogossypol,NSC736630 |
Others
|
|
(+)-Apogossypol is an antagonist of pan-BCL-2. (+)-Apogossypol binds to Mcl-1(Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively). |
|
T38810 |
BM-1197
|
|
|
|
BM-1197, a highly potent and specific dual inhibitor of Bcl-2 and Bcl-xL, effectively targets these proteins with IC50 values of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. This compound demonstrates notable an... |
|
T79171 |
Bcl-2-IN-11
|
|
|
|
Bcl-2-IN-11 (compound 6) is a potent and selective inhibitor of Bcl-2 activity, exhibiting an IC50 of 0.9 nM, and demonstrates minimal inhibition against Bcl-xl (IC50 > 1000 nM). This compound is utilized in researching ... |
|
T39909 |
XZ739
|
XZ739 |
|
|
XZ739 is a Cereblon-dependent PROTAC BCL-XL degrader, targeting a member of the Bcl-2 family, with a DC50 value of 2.5 nM in MOLT-4 cells after 16 hours of treatment. Additionally, XZ739 elicits cell death via caspase-me... |
|
T36883 |
BM-1074
|
|
|
|
BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM [1]. |
|
T26481 |
A-371191
|
A 371191 |
|
|
A-371191 is an antagonist of Bcl-XL. |
|
T36884 |
BM-1244
|
|
|
|
BM-1244 is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively. BM-1244 inhibits senescent fibroblasts (SnCs) with an EC50 of 5 nM[1]. |
|
T78988 |
A-1293102
|
|
|
|
A-1293102 is a potent, selective inhibitor of BCL-XL, effective in inducing apoptosis in tumor cells reliant on BCL-XL [1]. |
|
T40230 |
Mcl-1 inhibitor 6
|
|
|
|
Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compou... |
|
T40135 |
PZ703b
|
|
|
|
PZ703b is a novel BCL-XL PROTAC degrader with enhanced BCL-2 inhibition. |
|
T79377 |
NWP-0476
|
|
|
|
NWP-0476 is a modified BCL-2/BCL-xL inhibitor with enhanced specificity for BCL-xL, suitable for research on relapsed T-acute lymphoblastic leukemia (T-ALL) [1]. |
|
T39135 |
S65487 hydrochloride
|
S65487 hydrochloride,VOB560 hydrochloride |
|
|
S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is effective against BCL-2 mutations, including G101V and D103Y. It exhibits poor affinity for MCL-1, BFL-1, and BCL-XL. This compound induces apopto... |
|
T39701 |
Pomalidomide-C7-COOH
|
Pomalidomide-C7-COOH |
|
|
Pomalidomide-C7-COOH is a chemically synthesized E3 ligase cereblon ligand-linker conjugate, utilized as an intermediate compound for the synthesis of PROTAC BCL-XL degraders. |
|
T36901 |
Pelcitoclax
|
|
|
|
Pelcitoclax (APG-1252) is a powerful inhibitor of the Bcl-2 and Bcl-xl proteins, displaying significant antineoplastic and pro-apoptotic properties[1]. |
|
T40412 |
BAD (103-127) (human)
|
|
|
|
BAD (103-127) (human) is a 25-mer peptide obtained from the BH3 domain of BAD. It effectively counteracts the activity of Bcl-xL. Notably, BAD (103-127) (human) exhibits an approximately 800-fold greater binding affinity... |
