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 ǰȳ  Ű   Pharmacology

Apoptosis Small molecules

Apoptosis ʿ Small molecules Ұմϴ.

TOCRIS
ǰ ϱ
μϱ




Inhibitors
Cat. No. Product Name / Activity
5641 MSC 2032964A
Potent and selective ASK1 inhibitor; orally bioavailable
4429 NQDI 1
ASK1 inhibitor
4825 TC ASK 10
Potent and selective ASK1 inhibitor; orally bioavailable


Inhibitors
Cat. No. Product Name / Activity
2144 R18
Inhibitor of 14.3.3 proteins


Inhibitors
Cat. No. Product Name / Activity
2950 Acetyl-Calpastatin (184-210) (human)
Selective calpain inhibitor
0448 Calpeptin
Calpain and cathepsin L inhibitor
5208 E 64
Potent and irreversible cysteine protease inhibitor
1146 MDL 28170
Potent, selective calpain and cathepsin B inhibitor
3358 MG 101
Calpain inhibitor; activates p53-dependent apoptosis
1748 MG 132
Proteasome and calpain inhibitor. Inhibits NF-κB activation
1269 PD 150606
Cell permeable calpain inhibitor


Inducers
Cat. No.
Product Name / Activity
1229 Actinomycin D
Antineoplastic antibiotic
5330 AEG 40730 dihydrochloride
IAP antagonist; induces apoptosis
4846 Apicidin
Potent histone deacetylase inhibitor; induces apoptosis
2098 Apoptosis Activator 2
Selectively induces tumor cell apoptosis
3367 AT 101
Downregulates Bcl-2 and Mcl-1; pro-apoptotic
4810 BAM 7
Selective Bax activator; induces Bax-mediated apoptosis
3681 Bendamustine hydrochloride
Cytostatic agent; exhibits DNA alkylating and purine analog properties
3906 Betulinic acid
Antitumor and anti-HIV agent; activates NF-κB. Also TGR5 agonist
5372 Bioymifi
DR5 (TRAIL receptor) agonist; induces apoptosis
5791 Bz 423
ATP synthase inhibitor; proapoptotic
2489 C 75
Induces apoptosis and exhibits anti-tumor activity
2626 Carboplatin
DNA cross-linking antitumor agent
5144 CFM 4
CARP-1 mimetic; proapoptotic
5804 Chaetoglobosin A
Selectively induces apoptosis of CLL cells; antibiotic
3868 CHM 1
Potent antitumor agent; inducer of apoptosis
5800 CHMFL-FLT3-122
Induces apoptosis; FLT3 inhibitor
2251 Cisplatin
DNA-alkylating antitumor agent
5292 Cladribine
Deoxyadenosine analog; pro-apoptotic
5973 CP 724714
Potent and selective ErbB2 inhibitor; promotes tumor apoptosis
2841 Curcumin
Antitumor, anti-inflammatory and antioxidant
4091 Cyclophosphamide
Alkylating agent; chemotherapeutic
2137 2,3-DCPE hydrochloride
Selectively induces cancer cell apoptosis
1770 Deguelin
Anticancer and antiviral agent; chemopreventive and pro-apoptotic
2252 Doxorubicin hydrochloride
Antitumor antibiotic agent; induces apoptosis
4808 FK 866 hydrochloride
Potent and non-competitive NAMPT inhibitor; induces apoptosis and autophagy
3495 Fludarabine
Proapoptotic; increases Bax and decreases Bid, XIAP and survivin expression
3590 Gambogic acid
Apoptosis inducer. Activates caspases and inhibits Bcl-2 family proteins
3603 Kaempferol
Proapoptotic; downregulates PLK1 expression and activates mitochondrial Ca2+ uniporter
1807 2-Methoxyestradiol
Apoptotic and antiangiogenic agent
3258 Mitomycin C
DNA cross-linking antitumor agent
5231 MPC 6827 hydrochloride
Inhibitor of microtubule polymerization; antimitotic and antitumor
3715 Narciclasine
Antiproliferative agent; exhibits pro-apoptotic effects
4566 NSC 687852
Inhibitor UCHL5 and USP14; induces apoptosis
6026 Oleanolic acid
Selective GPBA receptor (TGR5) partial agonist; apoptosis inducer
3427 Oncrasin 1
Proapoptotic; induces abnormal nuclear accumulation of PKCι
2623 Oxaliplatin
DNA cross-linking antitumor agent
4643 PCI 34051
Potent and selective histone deacetylase 8 (HDAC8) inhibitor; induces apoptosis in T cell-derived cell lines
4396 Piperlongumine
Induces apoptosis; increases p53 and ROS levels in cancer cells
4761 Plumbagin
Induces apoptosis; anticancer
5359 Rifaximin
Apoptosis inducer; pregnane X receptor agonist and antibiotic
5314 SMBA 1
High affinity and selective activator of Bax
1621 Streptozocin
DNA alkylator; antitumor and induces diabetes
2706 Temozolomide
DNA-methylating antitumor agent
3909 Toceranib
Potent PDGFR and VEGFR inhibitor; induces apoptosis
4038 TW 37
Bcl-2 inhibitor; induces apoptosis


Inhibitors
Cat. No. Product Name / Activity
2172 AZ 10417808
Selective non-peptide caspase-3 inhibitor
2166 Z-DEVD-FMK
Cell-permeable, irreversible caspase-3 inhibitor
2168 Z-DQMD-FMK
Caspase-3 inhibitor
6172 INF 4E
Caspase-1 and NLRP3 inflammasome inhibitor
2163 Z-VAD-FMK
Cell-permeable, irreversible caspase inhibitor
Activators
Cat. No. Product Name / Activity
2251 Cisplatin
Potent pro-apoptotic anticancer agent; activates caspase-3
3590 Gambogic acid
Apoptosis inducer. Activates caspases
2581 PAC 1
Activator of procaspase-3; pro-apoptotic
1758 PETCM
Activator of caspase-3
Other
Cat. No. Product Name / Activity
2098 Apoptosis Activator 2
Promotes apoptosome formation and activates caspase-9/caspase-3 pathway. Selectively induces tumor cell apoptosis


Inhibitors
Cat. No. Product Name / Activity
6470 A 410099.1
High affinity XIAP antagonist; active in vivo
5141 AZD 5582 dihydrochloride
Dimeric Smac mimetic; potent IAP inhibitor
2156 Embelin
Inhibitor of X-linked inhibitor of apoptosis (XIAP); cell-permeable and antitumor
5251 UC 112
IAP and XIAP inhibitor; antitumor
6491 YM 155
Survivin suppressor
Other
Cat. No. Product Name / Activity
3253 Triptolide
Inhibits RNAPII-mediated transcription; antitumor, anti-inflammatory and immunosuppressive



Inhibitors
Cat. No. Product Name / Activity
6409 A 1210477
Selective, high affinity Mcl-1 inhibitor; proapoptotic
6960 ABT 199 
Selective, high affinity Bcl-2 inhibitor; orally bioavailable
6835 ABT 737 
Bcl-2 family inhibitor; mimics BH3 and induces apoptosis in cancer cell lines
4676 ARRY 520 trifluoroacetate
Potent and selective kinesin spindle protein (KSP) inhibitor; induces Mcl-1 degradation
2160 Bax channel blocker
Inhibits Bax-mediated mitochondrial cytochrome c release
1785 Bax inhibitor peptide V5
Inhibitor of Bax-mediated apoptosis
1787 Bax inhibitor peptide, negative control
Negative control peptide for Bax inhibitor peptide V5 (Cat. No. 1785)
6323 FX 1
Bcl-6 inhibitor; 10-fold more potent than endogenous Bcl-6 corepressors
3590 Gambogic acid
Apoptosis inducer. Inhibits Bcl-2 family proteins
1541 HA14-1
Bcl-2 inhibitor. Induces apoptosis
3794 iMAC2
Inhibitor of Bid-induced Bax cytochrome c release
5368 Maritoclax
Mcl-1 inhibitor; proapoptotic
4819 Methylprednisolone
Anti-apoptotic; upregulates expression of Bcl-xL after injury
4762 MIM1
Mcl-1 inhibitor; proapoptotic
5733 ML 311
Inhibits Mcl-1-BIM interaction
6539 Obatoclax mesylate
Inhibitor of Bcl-2 family members; antiapoptotic
4038 TW 37
Bcl-2 inhibitor; induces apoptosis
Activators
Cat. No. Product Name / Activity
4810 BAM 7
Selective Bax activator; induces Bax-mediated apoptosis
5314 SMBA 1
High affinity and selective activator of Bax
Other
Cat. No. Product Name / Activity
3367 AT 101
Downregulates Bcl-2 and Mcl-1; pro-apoptotic
3526 BIM, Biotinylated
Bim peptide fragment
2137 2,3-DCPE hydrochloride
Downregulates Bcl-XL protein expression
1964 Gossypol
Proapoptotic; downregulates Bcl-2 and Bcl-XL
3816 Muristerone A
Stimulates Bcl-XL mRNA transcription; antiapoptotic
2907 SU 9516
Transcriptionally downregulates Mcl-1; proapoptotic


Inhibitors
Cat. No. Product Name / Activity
1267 Pifithrin-α hydrobromide
p53 inhibitor. Also aryl hydrocarbon receptor agonist
3843 Cyclic Pifithrin-α hydrobromide
p53 inhibitor
2653 Pifithrin-μ
Inhibitor of p53-mitochondrial binding
Activators
Cat. No. Product Name / Activity
3503 HLI 373
Hdm2 inhibitor; activates p53-dependent transcription
6904 Idasanutlin 
Potent MDM2 inhibitor; inhibits MDM2-p53 interaction
6615 KCC 07
BAI1/p53 signaling activator; inhibits MBD2 (Methyl-CpG-binding domain protein 2)
2185 NSC 146109 hydrochloride
Cell-permeable, genotype-selective antitumor agent; activates p53-dependent transcription
5065 NSC 319726
Reactivator of mutant p53
2936 NSC 66811
MDM2 inhibitor. Disrupts MDM2-p53 interaction
3984 Nutlin-3
MDM2 antagonist; inhibits MDM2-p53 interaction
6075 Nutlin 3a
MDM2 antagonist; active enantiomer of Nutlin-3 (Cat. No. 3984)
2443 RITA
p53-MDM2 interaction inhibitor; antitumor
3929 SJ 172550
MDMX inhibitor. Disrupts MDMX-p53 interaction
5332 SP 141
High affinity MDM2 inhibitor
3365 Tenovin-1
Activates p53 transcriptional activity
3356 WR 1065 dihydrochloride
p53 activator. Also ROS scavenger
Other
Cat. No. Product Name / Activity
5417 BMH 21
p53 pathway activator; also RNA polymerase 1 inhibitor
3023 CP 31398 dihydrochloride
p53-stabilizing agent
3362 MIRA-1
Restores mutant p53 activity; proapoptotic
4326 PhiKan 083
p53 stabilizing agent
4396 Piperlongumine
Induces apoptosis; increases p53 and ROS levels in cancer cells
4761 Plumbagin
Induces p53 Ser10 phosphorylation; anticancer
1862 PRIMA-1
Restores mutant p53 activity; induces apoptosis
3710 PRIMA-1MET
Restores mutant p53 activity
3214 RETRA hydrochloride
Antitumor agent; suppresses mutant p53-bearing cancer cells
4240 SCH 529074
Restores mutant p53 activity